Journal of Applied Pharmaceutical Research

Polyherbal–antibiotic synergy: a review on mechanistic insights into polyphenols, flavonoids, alkaloids, and terpenoids for enhancing antimicrobial efficacy

2026-02-02T09:12:29+00:00

Background: Antimicrobial resistance (AMR) is one of the most important threats to global public health, accelerating as conventional antibiotics lose efficacy. Pathogens such as Staphylococcus aureus, Pseudomonas aeruginosa, Escherichia coli, and Klebsiella pneumoniae use a variety of resistance mechanisms, including enzymatic drug degradation, efflux pump activation, and biofilm formation. The declining pipeline of newly approved antibiotics highlights the need for alternative and adjunctive therapeutic strategies. Methodology: This review critically summarizes studies that analyze polyherbal–antibiotic combinations and their synergistic antimicrobial effects. A systematic review of recent literature on the role of phytochemicals, including alkaloids, flavonoids, terpenoids, tannins, and polyphenolic compounds, in potentiating antibiotic efficacy and reducing antibiotic resistance was conducted. Results and Discussion: Integrative synergetic interactions were strongly evidenced between antibiotics and plant-derived phytochemicals. Epigallocatechin gallate (EGCG) synergizes with β-lactam for common resistant strains, and berberine inhibits efflux pumps to enhance antibiotic activity. A wide range of flavonoids and polyphenolic extracts have been reported to exhibit antimicrobial activity, with mechanisms involving membrane disruption, biofilm inhibition, and interference with quorum-sensing pathways, thereby promoting multifaceted action. Conclusion: Synergy between polyherbal treatment and antibiotics is an innovative approach to combat AMR and should be prioritized. This approach highlights various leads for future antimicrobial therapeutics by combining traditional ethnopharmacological knowledge with innovative pharmaceutical paradigms.

Novel phytosomal drug delivery systems in cancer therapy: advances, mechanisms, and translational potential

2026-02-13T08:53:59+00:00

Background: Phytochemicals are medicinal plants with strong anticancer properties that alter various molecular pathways involved in tumor initiation, progression, and metastasis. Several adverse factors, however, hamper their clinical translation: low aqueous solubility, low membrane permeability, high first-pass metabolism, and rapid systemic elimination. Phytosomal drug delivery systems have emerged as a new, advanced lipid-based approach to addressing these pharmacokinetic and biopharmaceutical challenges. Methodology: Phytosomes are molecular complexes formed by a stoichiometric reaction between phytoconstituents and phospholipids, thereby increasing stability, improving bioavailability, and enhancing cellular uptake compared to conventional extracts and liposomal systems. Through meticulous analysis of articles from various publishers like PubMed, Science Direct, Elsevier, Bentham Science, Wiley, SAGE, Taylor and Francis publishers, and various indexing journals like Web of Sciences and Scopus databases, etc. Result and Discussion: This is a review of phytosomal technology in the treatment of cancers, including the principles of formulation, methods of preparation, physicochemical characterization, and the mechanisms of action of an increased anticancer effect. Conclusion: There is a critical discussion of preclinical and clinical evidence on phytosomal preparations of curcumin, silibinin, quercetin, catechins, and berberine. Further, present-day problems in translational research and regulation, as well as future opportunities, such as targeted and stimuli-responsive phytosomes, are also highlighted, indicating their potential as the next generation of phytomedicines in cancer therapy.

A scientific data-driven comprehensive review on seven prevalent species under Acacia (Fabaceae): insights into phytochemical investigation and pharmacological potentials

2026-02-13T05:36:16+00:00

Background: In traditional medicine, plants are important. For ages, various medicinal plants have been used for traditional medicine formulations, many of which are still in use today. There are many species under the genus Acacia that are important for medicine, most of which are found in Asia. Numerous species in the genus Acacia have long been used to treat a range of conditions, from mild ailments to serious cancers. Several species in this genus have been used in pharmaceutical and cosmeceutical formulations and have achieved commercial success due to their versatile medicinal properties. Methodology: The review followed the in-depth analysis of seven prevalent Acacia species. After screening an initial pool of approximately 500 articles on these species from sources such as PubMed and Scopus (2000–2026), around 120 publications were selected based on inclusion criteria (e.g., a focus on phytochemistry/pharmacology). This timeline highlights the novelty of the review while documenting emerging findings. Result and Discussion: Numerous studies in phytochemistry, pharmacology, and toxicology have demonstrated the positive therapeutic properties of substances such as betulin, catechin, diosgenin, kaempferol, and others for illnesses. In addition, numerous novel compounds with intriguing bioactivities have been disclosed by researchers. Conclusion: The species' pharmacological investigations and phytochemical analyses have been addressed and explained. In addition, botanical description and traditional applications are briefly discussed. The isolated compounds and their biological activities are discussed. All things considered, the genus Acacia emerges as a notable source of bioactive molecules with significant potential for pharmacognostical and drug development research in the years to come, especially in oncology.

Harnessing essential oils through nanotechnology-based drug delivery systems for biomedical applications: current trends and future prospects

2026-01-22T08:01:52+00:00

Background: Essential oils (EOs) have been used in therapeutic applications for centuries and continue to be popular in modern complementary and alternative medicine. EOs are highly concentrated, plant-derived volatile components with a wide range of biological activities, including analgesic, antibacterial, antifungal, antiviral, anti-inflammatory, and antioxidant activities. This study aims to review novel drug delivery systems enriched with essential oils to improve therapeutic outcomes, overcoming the limitations of the phytoconstituents, including high volatility, hydrophobicity, instability, and toxicity. Methodology: A literature review was conducted using globally recognized scientific research databases, including Google Scholar, PubMed, and Scopus. Studies were selected for their enhanced therapeutic applications of essential oils through novel drug delivery systems. The search strategy included keywords such as “essential oils”, “nanoformulations”, “nanoemulsions”, “liposomes”, and “solid lipid nanoparticles”, combined using Boolean operators (AND/OR). Articles published in English between 2021 and 2026 were considered. Result and Discussion: Encapsulation of EOs in nanocarriers and lipid-based vesicle systems enhances their bioavailability, improves their stability, and controls their release profile. The progressive nanotechnologies in the drug delivery system have advanced EO’s potential therapeutic approach for treating various disorders such as microbial diseases, pain, stomach disorders, depression, cancer, and many more. This review describes the potential of novel drug delivery systems to overcome the existing challenges associated with phytoconstituents. Conclusion: Novel drug delivery systems for EOs have the potential to improve the efficacy and safety of EO-based therapeutics. In this review, various novel drug delivery systems that have been reported to enhance the therapeutic potential of EOs by overcoming their limitations are highlighted.

Targeted nanocarriers for rheumatoid arthritis therapy: current evidence and translational barriers

2026-02-19T07:52:11+00:00

Background: Rheumatoid arthritis (RA) remains a debilitating autoimmune disorder characterized by chronic synovial inflammation and progressive joint destruction. Conventional systemic therapies provide symptomatic relief but often fail to achieve site-specific delivery, leading to adverse effects and limited long-term efficacy. This review appraises the available evidence for the use of targeted nanocarrier drug delivery systems in the treatment of RA and highlights the translational hurdles that hinder their clinical use. Methodology: A search of PubMed, Scopus, and Web of Science (2015-2025) was conducted using the keywords RA, nanocarriers, liposomes, polymeric nanoparticles, and microneedles. Result and Discussion: Liposomal and polymeric nanoparticle systems are emerging nanotechnologies that have demonstrated improved targeting and therapeutic outcomes in preclinical models. In addition, microneedle technologies show potential for less painful delivery through the skin. Conclusion: Despite encouraging results, inconsistent manufacturing reproducibility, limitations in large-scale production, and regulatory uncertainties, among others, remain factors that are slowing the transition to the clinic. Standardization of characterization procedures, validated preclinical models, and well-designed translational research are among the measures this review has identified as necessary to facilitate the transition of nanocarrier-based therapeutics to clinical application in RA.

Comparative pharmacological and clinical review of selected herbal antihypertensive agents in hypertension management

2026-04-23T18:20:12+00:00

Background: Hypertension is a major global health concern and a leading risk factor for cardiovascular morbidity and mortality. Limitations associated with conventional antihypertensive therapy, including poor compliance, adverse effects, and inadequate blood pressure control, have increased interest in herbal agents possessing multitarget pharmacological actions and improved safety profiles. Methodology: A comparative literature review was conducted using PubMed, Scopus, Web of Science, Google Scholar, and ScienceDirect databases to identify relevant studies published between 2020 and 2026. Approximately 130 articles were screened, of which 80 relevant experimental studies, clinical trials, and meta-analyses were included for comparative evaluation of the antihypertensive effects, mechanisms, phytochemical profiles, and clinical relevance of selected herbal agents. Result and Discussion: Garlic (Allium sativum) demonstrated the strongest clinical evidence with consistent reductions in systolic and diastolic blood pressure through ACE inhibition, nitric oxide enhancement, and antioxidant effects. Ginger (Zingiber officinale) showed predominantly experimental evidence, with limited clinical evidence, of calcium channel blockade and vascular relaxation. Rauwolfia serpentina exhibited potent antihypertensive efficacy but was limited by neuropsychiatric adverse effects, whereas Terminalia arjuna provided moderate antihypertensive and cardioprotective benefits. Conclusion: Herbal antihypertensive agents exhibit mechanism-specific and stage-dependent therapeutic potential and may serve as supportive interventions in early-stage hypertension and cardiovascular comorbidities. However, the lack of standardization and limited long-term clinical evidence remain major limitations that require further investigation.

Development, in-vitro and ex-vivo evaluation of HPMC E-15/Xanthan gum mucoadhesive buccal patch of telmisartan

2026-01-17T05:47:59+00:00

Background: Telmisartan, an antihypertensive drug, exhibits poor aqueous solubility and low oral bioavailability due to extensive hepatic first-pass metabolism. Buccal delivery offers a potential alternative route to bypass first-pass metabolism and achieve sustained drug release for better blood pressure control, particularly in nocturnal hypertension. The aim of the work was to formulate and evaluate a Telmisartan mucoadhesive buccal patch for sustained drug delivery. Methodology: Telmisartan solid dispersion with Kolliphor RH 40 was prepared by solvent evaporation, and mucoadhesive buccal patches (T1–T9) were formulated by solvent casting and optimized using a 3² full factorial design with Xanthan gum (A) and HPMC E15 (B) at three levels each, followed by evaluation of physicochemical properties, mucoadhesion, swelling, drug release, permeation, and drug–excipient compatibility by FT-IR, DSC, and XRD. Results & Discussion: Based on statistical analysis, it was observed that Xanthan gum and HPMC E15 significantly (p < 0.05) affected all the responses, and T9 was selected as the optimized formulation with a desirable swelling index of 331% and strong mucoadhesive strength of 28.5 ± 0.5 g. Optimized formulation T9 showed sustained drug release of 94.87%, and ex vivo permeation of 1.773 ± 0.033 mg/cm²) with a flux of 0.221 mg/cm²/h). Conclusion: The optimized T9 patch exhibited enhanced swelling, adhesion, sustained release, and permeation, suggesting its potential as an effective alternative for managing nocturnal hypertension.

AQbD assisted UPLC method development and validation of tirzepatide in bulk and pharmaceutical dosage form

2026-02-04T05:25:36+00:00

Background: Tirzepatide is a USFDA-approved (2023) synthetic drug that primarily targets blood sugar metabolism for chronic weight management, obesity-related conditions, and type 2 diabetes. In this study, we aim to develop a reliable, sensitive UPLC method for estimating Tirzepatide using Analytical Quality by Design (AQbD) to optimize chromatographic conditions. Methodology: The finalized method was developed using the Agilent 1290 Infinity II LC System, with a Phenomenex C18 column (50 x 1.7 mm, 2.1 µm), using a mobile phase of acetonitrile and trifluoroacetic acid buffer (37.07:62.93, v/v) at a flow rate of 0.57 mL/min and a Photo Diode Array detector at 264 nm. Result and Discussion: The method validation showed linearity over the range of 12.5–75 µg/mL (R² = 0.9995). The intraday and interday precision (%RSD) values were 0.603 and 0.791, respectively, confirming the method's reproducibility. Limit of Detection and Limit of Quantification values were calculated from S/N ratios of the prepared samples and were 0.6 and 2, respectively. Accuracy was validated to be 99.3-101.1%. The forced degradation studies were conducted under stress conditions, including acid, alkali, peroxide, reduction, photodegradation, and hydrolysis, with tirzepatide showing degradation percentages of 1.3%, 11.3%, 12.1%, 2.1%, 1.7%, and 2.9%. Conclusion: The developed UPLC method for quantifying tirzepatide was found to be significant, with all evaluated parameters in agreement with ICH guidelines. The proposed method is efficient, straightforward, and dependable, rendering it appropriate for routine quality control of tirzepatide in bulk and pharmaceutical formulations

Formulation and evaluation of SPAN-60-based valacyclovir proniosomal gel for ocular delivery

2026-02-04T10:28:04+00:00

Background: Ocular administration is a challenging route of drug delivery due to the eye's distinct anatomy and physiology. Valacyclovir is commonly prescribed to treat viral ophthalmological conditions. However, its poor permeability limits its effectiveness in ocular viral infections. In this study, valacyclovir proniosomal gels (F1-F14) have been prepared for ocular permeation. Methodology: The VCV proniosomal gel was prepared using varying ratios of cholesterol, Span 60, and lecithin via coacervation-phase separation. The prepared proniosomal gels were characterized for particle size and shape, viscosity, drug entrapment efficiency (EE%), surface morphology, zeta potential, and in vitro drug release. Result and Discussion: Data from experimentation indicate that all formulations prepared were found to have high entrapped efficiency (%), with the highest value being (90.70%) for F7. The final formulation showed a ZP of -27.40 ± 2 mV, a PDI of 0.231, and a vesicle size of 64.31 nm, indicating uniformly dispersed, nanosized vesicles well-suited for ocular drug delivery and exhibiting greater colloidal stability. Conclusion: The results from all fourteen formulations of in vitro drug release demonstrated that they all released their drug in a sustained manner for at least 10 hours following release. The patterns of drug release from the in vitro tests fitted into the Korsmeyer–Peppas model of drug release kinetics. Overall, the results show that using VCV in a proniosomal form enables prolonged, enhanced corneal permeation.

Phytochemical evaluation and in-vitro anti-bacterial and antioxidant effect of extract of Solanum xanthocarpum and Achyranthes aspera

2026-02-04T08:14:40+00:00

Background: This study investigates the phytochemical composition, antioxidant activity, and antibacterial properties of extracts from Solanum xanthocarpum and Achyranthes aspera. Achyranthes aspera exhibited 65.864 % inhibition with an IC50 value of 31.056 µg/mL, and Solanum xanthocarpum showed 55.385% inhibition with an IC50 value of 51.920 µg/mL. Methodology: The total phenolic content (TPC) and total flavonoid content (TFC) were measured using the Folin-Ciocalteu assay and aluminum chloride colorimetric method, respectively. Antioxidant activities were evaluated using DPPH radical-scavenging and reducing power assays. The antibacterial activity against Streptococcus mutans was determined using the well diffusion method. Result and Discussion: The TPC of Solanum xanthocarpum and Achyranthes aspera extracts were 77.80 mg GAE/g and 98.40 mg GAE/g, respectively, while the TFC were 82.66 mg RE/g and 136.66 mg RE/g. In the DPPH assay, Achyranthes aspera exhibited 65.864 % inhibition with an IC50 value of 31.056 µg/ml, and Solanum xanthocarpum showed 55.385% inhibition with an IC50 value of 51.920 µg/mL. The reducing power assay indicated significant antioxidant potential, especially for Achyranthes aspera. The antibacterial activity against Streptococcus mutans MTCC 389 revealed that Achyranthes aspera exhibited a maximum inhibition zone of 23±1.732 mm. At the same time, Solanum xanthocarpum showed a maximum inhibition zone of 20±1 mm at a concentration of 2 mg/mL. Conclusion: The extracts of Solanum xanthocarpum and Achyranthes aspera demonstrate significant antioxidant and antibacterial activities, highlighting their potential as natural sources of antimicrobial and antioxidant agents. Further research is needed to isolate bioactive components, elucidate their mechanisms of action, and assess their potential cytotoxic effects on human cells.

Design and characterization of a mucoadhesive nanoparticle-loaded thermo-responsive in-situ nasal gel for enhanced brain delivery of an antimigraine drug

2026-01-26T00:33:18+00:00

Background: Migraine is a debilitating neurological disorder that requires rapid and effective drug delivery to the brain. Conventional oral and parenteral therapies are associated with delayed onset of action, low patient compliance, limited central nervous system (CNS) bioavailability due to the blood-brain barrier (BBB), and hepatic first-pass metabolism. This study aimed to develop a thermoresponsive, mucoadhesive, nanoparticle-loaded nasal in situ gel to enhance brain delivery of an antimigraine drug. Methodology: Drug-loaded nanoparticles were prepared via ionic gelation and incorporated into a thermo-sensitive nasal in situ gel via the cold method. Results and Discussion: The optimized nanoparticle formulation (NP13) exhibited a small particle size (154.3 nm), acceptable polydispersity index (0.3485), positive zeta potential (22.79 mV), high entrapment efficiency (89.09%), drug loading (14.33%), and sustained drug release (90.26%). The developed in situ gel showed optimal pH (6.8), suitable gelling temperature (28–34 °C), viscosity (556 cp), entrapment efficiency (85%), drug content (95.82%), in vitro drug release (88.89 ± 0.98%), and ex vivo permeation (85.24 ± 0.67%) over 10 hours. Histopathological studies confirmed minimal nasal mucosal irritation compared to the drug solution and isopropyl alcohol. MTT assay results demonstrated concentration-dependent cytotoxicity, with SS-NPs ISG4 showing higher cell viability than the free drug, indicating reduced cytotoxicity due to nanoparticle encapsulation. Blank nanoparticles exhibited maximum cell survival, confirming carrier biocompatibility. Conclusion: The developed nanoparticle-loaded nasal in situ gel demonstrated promising safety, biocompatibility, and enhanced delivery potential, validating its suitability for intranasal migraine therapy.

Quinoxaline amino derivatives as potential EGFR-targeted therapeutics in breast cancer: computational exploration

2025-12-24T18:54:36+00:00

Background: Despite resistance to current tyrosine kinase inhibitors, which makes the epidermal growth factor receptor (EGFR) a recognized therapeutic target in breast cancer, there is a need for novel inhibitors. Quinoxaline compounds are a promising scaffold for next-generation EGFR inhibitors and exhibit favorable pharmacological properties. Methodology: Ten new amino quinoxaline derivatives (QN1–QN10) were systematically developed and assessed by a comprehensive in silico approach. Molecular docking was conducted on the EGFR tyrosine kinase domain (PDB ID: 4HJO) utilizing Glide XP, with erlotinib serving as the reference ligand. Drug-likeness, oral bioavailability, and synthetic accessibility were evaluated using SwissADME, whereas pkCSM predicted ADMET characteristics. The most effective candidate was subsequently corroborated by 100 ns molecular dynamics (MD) simulations utilizing GROMACS 2021.1, succeeded by MM-GBSA binding free energy assessments. Results and Discussion: According to docking data, QN8 proved the most promising inhibitor. It showed stable hydrogen bonding with key EGFR hinge residues (MET769 and ASP831) and a high binding affinity (−9.305 kcal/mol), comparable to erlotinib (−9.501 kcal/mol). Consistent RMSD and RMSF profiles from MD simulations corroborated the structural stability of the QN8–EGFR complex. According to MM-GBSA analysis, the van der Waals, lipophilic, and electrostatic contributions were the main drivers of the favorable binding free energy (-73.63 kcal/mol). Pharmacokinetic predictions showed adequate ADMET properties and good oral absorption. Conclusion: This exhaustive computational analysis highlights amino quinoxaline derivatives as promising leads for developing breast cancer drugs, identifying QN8 as a strong EGFR inhibitor with stable binding dynamics and favorable drug-like properties.

Formulation and characterization of risperidone nanocrystals for enhanced solubility and dissolution

2026-02-18T08:01:47+00:00

Background: Risperidone (RIS) is categorized as a BCS Class II antipsychotic and exhibits poor water solubility and a slow dissolution rate, which restricts its therapeutic effectiveness. The present study aims to formulate RIS nanocrystals to overcome pharmaceutical challenges and improve their solubility. Methodology: Nanosuspensions of RIS were prepared using high-speed homogenization, with different polymer ratios. The physicochemical properties were characterized using FTIR, SEM, particle size analysis, zeta potential measurement, X-ray powder diffraction, entrapment efficiency evaluation, drug content analysis, and in vitro release testing. Direct compression was used to manufacture tablets from the optimized nanocrystals, and their dissolution performance was assessed against conventional RIS tablets. Results and Discussion: The formulation F7, containing 0.1% Poloxamer 188 and prepared at 25,000 rpm, exhibited the optimal particle size (78.62 nm), PDI (0.223), and zeta potential (-18.9 mV), and the SEM images revealed needle-shaped crystals. Entrapment efficiency was 86.22±1.61% with a drug content of 67.885±2.02%. The F7 nanosuspension released 90.23±1.91% of the drug in phosphate buffer (pH 6.8) within 60 minutes. Reducing the size of nanoscale particles enhanced their surface area, hence increasing their solubility. The F7 nanocrystal tablets released 86.28±1.83% of the drug, whereas the conventional tablets released 77.51±2.15%. This data demonstrates that this method is more effective. Conclusion: RIS nanocrystals were developed to enhance solubility and accelerate dissolution rates. The F7 formulation exhibited enhanced stability and improved release, suggesting its potential to optimize oral medication delivery.

Isolation, alkaline extraction, and characterization of starch from mango seeds for pharmaceutical applications

2026-02-04T05:01:49+00:00

Background: Mango (Mangifera indica L.) seed is an abundant agro-waste with potential as a sustainable biopolymer source. This study explores the conversion of mango seed waste into high-purity starch and evaluates its physicochemical, structural, and functional properties for pharmaceutical applications. Methodology: The starch extracted from mango seeds by the alkaline method was subjected to phytochemical screening, physicochemical evaluation, flow property analysis, and advanced characterization techniques, including ATR-FTIR, NMR, SEM, XRD, DSC, and mass spectrometry. Results and discussion: The extraction process yielded 40% (w/w) starch. Phytochemical screening confirmed the exclusive presence of carbohydrates, indicating high purity. The starch exhibited a high amylopectin content (98.47%) and a low amylose content (1.53%), indicating a highly branched structure. Moisture content was low (0.80%), while the swelling index reached 180%, demonstrating excellent water absorption. The pH was slightly acidic (6.12 ± 0.07), and flow properties were acceptable based on bulk density, tapped density, Carr’s index, and Hausner’s ratio. SEM showed oval and irregular granules sized 10–22 μm. ATR-FTIR and NMR confirmed polysaccharide structures, XRD revealed A-type crystallinity, DSC showed thermal degradation at 326 °C with an enthalpy of 29.63 J/g, and mass spectrometry indicated glucose polymer fragmentation. Conclusion: Mango seed starch demonstrates high purity with trace residual lipids/proteins detected by spectroscopic analysis, favorable functional properties, and structural stability, supporting its potential as a sustainable and effective excipient for pharmaceutical formulations.

Development and optimization of a mechlorethamine topical formulation utilizing a model drug bridging strategy and quality by design

2026-01-26T11:25:52+00:00

Background: This study aimed to develop a stable, clinically suitable topical mechlorethamine formulation using Quality by Design (QbD) principles to address chemical instability and cytotoxicity. The objectives were to establish a data-driven formulation design space, identify critical material attributes, and apply a surrogate active pharmaceutical ingredient (API) approach to ensure biological performance while enabling safe early-stage optimization. Methodology: A 2³ full factorial Design of Experiments (DOE) was employed to evaluate the effects of ethanol, isopropyl myristate (IPM), and Carbopol 974P on assay concentration, viscosity, and pH. Regression modeling and response surface analysis were used to define the formulation design space. Diclofenac sodium was used as a surrogate API to study matrix behavior prior to the incorporation of mechlorethamine. The optimized formulation was subjected to long-term, refrigerated, and accelerated stability studies. Results and Discussion: Carbopol 974P concentration was identified as the primary factor influencing viscosity, while assay concentration and pH remained stable across the design space. The optimized formulation (73% ethanol, 3% IPM, and 0.12% Carbopol 974P, pH 5.5) met all Quality Target Product Profile criteria. Bridging studies demonstrated comparable physicochemical properties between surrogate and mechlorethamine-loaded formulations, indicating excipient-driven performance. Under ICH stability conditions, the optimized formulation retained 98.3% assay after 3 months at 40°C/75% RH (0.9% loss), with total impurities remaining at 0.19% (NMT 0.5%), stable viscosity (40–60 cps), controlled pH (5.51–5.53), and no physical instability. Conclusion: The QbD-driven approach enabled the development of a stable, reproducible, and biologically effective topical mechlorethamine formulation suitable for scale-up and regulatory advancement.

Design, synthesis, and in silico evaluation of 1,4 dihydropyridine and 3,4 dihydropyrimidine 2(1H)-ones/thione derivatives

2026-01-24T10:43:06+00:00

Background: Pyridine and pyrimidine derivatives occupy a central position in medicinal chemistry owing to their broad pharmacological significance. In particular, 1,4-dihydropyridines and 3,4-dihydropyrimidines are known for their anti-hypertensive and anti-anginal activities, encouraging further exploration of their chemical space. Methodology: This study aimed to design and synthesize a novel series of nineteen derivatives (PS-1 to PS-19) based on 1,4-dihydropyridine and 3,4-dihydropyrimidine-2(1H)-ones/thiones, employing a green synthetic strategy. The pharmacological viability of these compounds was assessed through in silico profiling. A catalyst-free "on-water" approach was used for synthesis, aligning with green chemistry principles to ensure eco-friendliness, operational simplicity, and high yield. Structural elucidation of the synthesized compounds was performed using infrared (IR) and proton nuclear magnetic resonance (^1H NMR) spectroscopy. Purity was assessed via thin-layer chromatography (TLC). Pharmacological activity, physicochemical properties, and toxicity profiles were evaluated using PASS Online, Swiss ADME, and Protox-II. Results and Discussion: Among the compounds screened, PS-4 demonstrated the most favorable docking affinity (−49.20), outperforming benchmark calcium channel blockers such as Nifedipine and Felodipine. The developed green synthetic method successfully yielded 19 target compounds with desirable purity and structural fidelity. Three compounds out of 19 showed a strong docking score towards the receptor protein. Conclusion: In silico results revealed favorable pharmacological potential and acceptable toxicity margins for several derivatives, suggesting they are promising candidates for further pharmacodynamic and therapeutic investigations.

Analytical profiling and antioxidant characterization of flavonoids from himalayan black soybean (Glycine max)

2026-02-09T07:09:46+00:00

Background: Black soybean is a leguminous crop of great phytochemical interest and importance in traditional systems due to its alleged health-promoting effects. To a great extent, these advantages are attributed to its flavonoid content, a class of polyphenols known for their strong antioxidant properties. This research was part of a significant task: conducting a comprehensive phytochemical characterization of the flavonoid profile in black soybean seeds and assessing their respective antioxidant potential in vitro. Methodology: Flavonoids were extracted from authentic seeds using 70% aqueous ethanol. UV-Vis, FTIR, and 1H NMR spectroscopy were used to elucidate the extract's functional groups and structure. Specific flavonoids (rutin, quercetin) were analyzed quantitatively by use of validated HPLC. In the determination of total flavonoid content, a spectrometric method was used. The DPPH radical-scavenging assay was used to determine antioxidant activity. Results and Discussion: Spectroscopic studies revealed the presence of typical flavone/flavonol skeletons. The HPLC quantification illustrated good method performance. The TFC was 5.91 mg QE/g extract. The extract exhibited high dose-dependent scavenging activity against the DPPH radical. High TFC was strongly correlated with antioxidant activity, confirming the bioactive capacity of black soybean, known for its flavanol-rich flavonoids. Conclusion: The results are scientifically confirmed: black soybean is rich in bioactive flavonoids with high antioxidant capacity and can therefore be used as a functional food ingredient or nutraceutical to treat oxidative stress.

Kaempferol-rich Thespesia lampas leaf extract mitigates gentamicin-induced nephrotoxicity via antioxidant and anti-inflammatory mechanisms in wistar rats

2026-01-20T06:36:18+00:00

Background: Gentamicin-induced nephrotoxicity (GIN) is a major limitation of aminoglycoside therapy and a common cause of acute kidney injury (AKI). The underlying mechanisms involve excessive oxidative stress and activation of inflammatory signaling pathways, particularly the nuclear factor-κB (NF-κB) pathway. Natural flavonoids such as kaempferol possess strong antioxidant and anti-inflammatory properties. Thespesia lampas, traditionally used in renal disorders, is rich in kaempferol, necessitating scientific validation of its nephroprotective potential. Methodology: ALE was characterized using HR-LCMS, confirming kaempferol as the major flavonoid (20.5 ± 2.8 mg/g extract; 2.05 ± 0.28% w/w). Antioxidant activity was assessed by the DPPH assay, demonstrating potent free radical scavenging (IC₅₀ = 62.4 µg/mL) comparable to rutin standard (IC₅₀ = 48.6 µg/mL). Rats received ALE orally at doses of 100, 200, and 400 mg/kg for 28 days, while nephrotoxicity was induced by gentamicin (50 mg/kg/day, i.p.) during the final 10 days. Renal function markers, oxidative stress parameters, pro-inflammatory cytokines (TNF-α, IL-6), NF-κB (p65/p50) nuclear translocation, and renal histopathology were evaluated. Results and Discussion: Gentamicin caused significant renal dysfunction, oxidative imbalance, elevated inflammatory cytokines, and increased NF-κB activation. ALE treatment produced dose-dependent nephroprotection, with the 400 mg/kg dose markedly restoring renal biomarkers, improving antioxidant defenses, suppressing inflammatory mediators, and ameliorating histopathological damage. Conclusion: Kaempferol-rich Thespesia lampas ALE confers significant protection against gentamicin-induced nephrotoxicity by attenuating oxidative stress and inhibiting NF-κB–mediated inflammation, highlighting its potential as a therapeutic agent for drug-induced renal injury.

Formulation and evaluation of metformin-loaded microspheres using modified double emulsion solvent evaporation technique

2026-01-15T06:14:35+00:00

Background: Metformin hydrochloride is the first-line therapy for Type 2 diabetes mellitus; however, its short biological half-life, low oral bioavailability, and frequent dosing often compromise patient compliance and cause gastrointestinal side effects. Sustained-release delivery systems may overcome these limitations. This study aimed to develop and evaluate ethylcellulose-based sustained-release metformin-loaded microspheres using a modified W/O/W double-emulsion solvent evaporation technique. Methodology: Six formulations (MF-M1 to MF-M6) were prepared by varying ethylcellulose concentrations (1.0–3.5% w/v). Microspheres were evaluated for percentage yield, entrapment efficiency (EE%), particle size, swelling index, surface morphology (SEM), thermal behavior (DSC), drug–polymer compatibility (FTIR), in-vitro drug release, and release kinetics. Results and Discussion: Increasing ethylcellulose concentration significantly improved yield (65.4–88.2%) and EE% (58.2–85.6%) while increasing particle size (48.2–121.5 µm). MF-M5 (3% EC) demonstrated optimal performance with high yield (85.6%), EE% (82.1%), controlled initial burst (7.2%), and sustained release (91.6% over 24 h). MF-M6 exhibited the longest release but showed a larger particle size and processing challenges. Drug release followed first-order and Higuchi kinetics, with anomalous transport observed at higher polymer levels. Conclusion: The modified W/O/W technique successfully encapsulated hydrophilic metformin into sustained-release microspheres. MF-M5 is identified as the most balanced formulation, while MF-M6 may be suitable where maximum release retardation is required.

An in silico network pharmacology and molecular dynamics simulations study of engeletin in ischemic stroke with computational prioritisation of NOS2

2026-01-09T01:49:01+00:00

Background: Engeletin, a polyphenolic flavonoid, has demonstrated neuroprotective effects in experimental stroke models. However, the molecular interactome underlying its multitarget actions in ischemic stroke remains insufficiently characterized. Methodology: An integrated in silico workflow was applied to identify stroke-relevant targets of engeletin, combining target prediction, protein–protein interaction analysis, GO and KEGG pathway enrichment, and engeletin–target–pathway network construction. Network topology metrics were used to prioritize targets for downstream structure-based analyses. Docking was performed on short-listed targets, and selected protein–ligand complexes were further evaluated using molecular dynamics (MD) simulations to assess binding stability. In silico ADME profiling was conducted to contextualize translational considerations. Results and Discussion: Nineteen targets were identified through a confidence-driven overlap strategy. Degree-based network filtering short-listed 11 targets for docking. Multi-centrality convergence across protein–protein interaction and engeletin–target–pathway networks prioritized six influential hubs (PTGS2, CASP3, NOS2, MMP9, JAK2, and EGFR) implicated in inflammatory, apoptotic, and vascular regulation. Functional enrichment analyses highlighted interconnected inflammatory–immune, vascular, and metabolic stress pathways, with KEGG pathways interpreted as nominally enriched. Docking and MD analyses differentiated dynamically stable interactions from network-level co-modulated hubs, with engeletin exhibiting the most stable binding to NOS2 (inducible nitric oxide synthase). Conclusion: Integration of network pharmacology with structure-based analyses prioritizes NOS2-centered modulation and relaxin-associated vascular signaling as testable mechanisms for future experimental validation of engeletin in ischemic stroke.

Acute toxicity evaluation and antidyslipidemic potential of Retama sphaerocarpa aerial parts in Triton WR-1339 induced hyperlipidemic rats

2026-02-03T09:07:12+00:00

Background: Dyslipidemia constitutes a major risk factor for cardiovascular diseases. Although conventional lipid-lowering therapies are effective, their prolonged use is associated with adverse effects, highlighting the need for safer natural alternatives. Species of the genus Retama, including Retama sphaerocarpa, have been reported to possess various pharmacological properties, including antioxidant, hepatoprotective, anti-inflammatory, and hypoglycemic activities. However, no study to date has evaluated the antidyslipidemic potential of R. sphaerocarpa. This study was conducted to evaluate both the acute oral toxicity and the antidyslipidemic effect of the Retama sphaerocarpa aqueous extract (RSAE) in a Triton WR-1339-induced hyperlipidemic rat model. Methodology: The acute toxicity study of RSAE was conducted in accordance with OECD Guideline 423. RSAE was administered orally as a single dose of 2000 mg/kg, and the rats were monitored for any signs of toxicity or mortality. Hematological and biochemical parameters were assessed 24h post-administration of RSAE. The antidyslipidemic effect of RSAE (400 mg/kg) was studied in Triton WR-1339-induced dyslipidemia in Wistar albino rats. Results and discussion: Results showed no mortality or clinical signs of toxicity following RSAE administration; hematological and biochemical parameters remained unaltered after 24 hours post-treatment. The RSAE demonstrated antioxidant activity (IC₅₀ = 241.45 μg/mL). For the lipid-lowering assessment, RSAE pretreatment significantly reduced plasma TC levels by 51.1% (p<0.01), TGs by 60.2% (p<0.01), and LDL-c by 73.5% (p<0.01), while increasing HDL-c levels (p<0.01). Conclusion: Results from the present study highlight the potential of Retama sphaerocarpa in the prevention and management of dyslipidemia.

Vanillin as a cardioprotective agent against anthracycline-induced cardiotoxicity in Wistar rats via modulation of oxidative stress and molecular docking analysis

2026-01-17T06:06:48+00:00

Background: Doxorubicin (DOX) is limited by dose-dependent cardiotoxicity mediated by reactive oxygen species (ROS) and oxidative stress. Natural phenolic compounds, such as vanillin, with antioxidant properties, are being explored as cardioprotective agents. This study evaluated vanillin using integrated in silico and in vivo approaches. Methodology: Molecular docking assessed vanillin–cardiac protein interactions, and ADMET profiling evaluated drug-likeness. In vivo, DOX-induced cardiomyopathy was established in male Wistar rats (n=6) via cumulative intraperitoneal dosing (16 mg/kg). Vanillin (50, 100, and 200 mg/kg) was administered orally 30 minutes post-DOX for 28 days. ECG parameters, cardiac biomarkers (CK-MB, AST, LDH, cTn-I), oxidative stress markers (MDA, SOD, GSH, catalase), and histopathology were analyzed. Results & Discussion: In silico analysis revealed that vanillin binds to the CK-MB active site, demonstrating a docking interaction comparable to that of doxorubicin. In vivo, Doxorubicin treatment caused significant cardiac dysfunction, characterized by QTc prolongation and ST-segment depression. Serum biomarkers of myocardial injury (CK-MB, Troponin-I, LDH, AST) were significantly elevated, while myocardial antioxidant levels (SOD, GSH, CAT) were depleted in the DOX group. Vanillin co-administration (200 mg/kg) significantly attenuated these alterations, restoring QTc intervals and reducing oxidative stress markers. Histopathological scoring confirmed improving myocardial architecture from severe damage in the DOX group to near-normal morphology in the high-dose Vanillin group. Conclusion: Vanillin exerts cardioprotective effects via antioxidant mechanisms, stabilization of cardiac biomarkers, and maintenance of myocardial integrity, indicating its promise as an adjunct strategy against anthracycline-induced cardiotoxicity.

Therapeutic potential of mesalamine-probiotic combination in enteric-coated tablet for modulating gut inflammation in IBD

2025-10-07T10:53:10+00:00

Background: Mesalamine is widely used for inflammatory bowel disease (IBD) due to its local anti-inflammatory action, while probiotics help restore intestinal microbiota and modulate immune responses. Combining both may offer synergistic benefits for IBD management. This study aimed to develop and evaluate colon-targeted enteric-coated tablets containing a mesalamine-probiotic combination. Methodology: Core tablets containing mesalamine, selected probiotics, and polymers were prepared by dry granulation. Pre- and post-compression parameters were evaluated. The optimized batch was coated with Eudragit® S100 (2–5%) to achieve pH-dependent release. In vitro dissolution and probiotic viability in simulated gastric conditions were assessed. Result and Discussion: The optimized formulation showed acceptable physical properties and negligible drug release in gastric pH, followed by targeted colonic release exceeding 90% at intestinal/colonic pH. Mesalamine release followed Higuchi kinetics, suggesting diffusion-controlled behavior. Swelling studies demonstrated gradual polymer hydration and matrix erosion. Probiotic viability studies demonstrated strain-dependent survival: Saccharomyces boulardii and Streptococcus thermophilus retained>90% viability after 150 min of simulated gastric exposure, whereas Lactobacillus acidophilus and Bifidobacterium bifidum exhibited approximately 1.2–1.3 log reductions, indicating greater acid sensitivity. The combination of enteric coating enabled efficient colon targeting and sustained release. Differential strain viability emphasized the importance of selecting acid-resistant probiotics or employing protective delivery systems. Conclusion: The developed mesalamine–probiotic enteric-coated tablets demonstrated colon-specific drug release and strain-dependent probiotic survival in vitro, indicating their potential as a candidate formulation requiring further optimization, particularly for acid-sensitive bacterial strains.

AQbD enabled optimization of RP-HPLC method for the estimation of pioglitazone and vildagliptin and its forced degradation studies

2025-11-14T04:11:37+00:00

Background: Diabetes mellitus is a metabolic disorder that is managed with combination therapy. Pioglitazone improves insulin sensitivity by activating PPAR-γ, whereas vildagliptin increases incretin activity by inhibiting DPP-4. Their fixed-dose combination requires reliable analytical methods for quality control and stability assessment. This study aimed to develop a green, stability-indicating RP-HPLC method using the Analytical Quality by Design (AQbD) approach. Methodology: A systematic AQbD strategy employing Central Composite Design (CCD) with 13 experimental runs was used to optimize critical analytical parameters. Chromatographic separation was performed on an Agilent 1260 Infinity II HPLC system using a Phenomenex C18 column (150 × 4.6 mm, 5 µm). Detection was carried out at 220 nm with a flow rate of 0.8 mL/min. The method was validated in accordance with ICH guidelines, and greenness was evaluated using the AGREE, MoGAPI, and BAGI metrics. Results and Discussion: Vildagliptin and pioglitazone were well resolved with retention times of 2.21 min and 3.47 min, respectively. Validation results demonstrated excellent precision, accuracy, and reliability. The method exhibited acceptable greenness with a high BAGI score of 82.5, an AGREE score of 0.66, and a MoGAPI value of 74. Stress degradation studies confirmed its stability-indicating capability, with maximum degradation under alkaline and oxidative conditions, while acidic, thermal, and photolytic stresses showed minimal effects. Conclusion: The proposed AQbD-driven, eco-friendly RP-HPLC method is sensitive, stability-indicating, and regulatory-compliant, offering reduced analysis time, enhanced robustness, and improved environmental performance, making it a sustainable and efficient approach for routine estimation of pioglitazone and vildagliptin.

Formulation and comparative evaluation of allopurinol transdermal patches using two different polymeric combinations

2025-12-16T08:46:21+00:00

Background: The transdermal drug delivery system is a technique where drugs are absorbed via the skin at a predetermined and controlled rate. This system offers several benefits over conventional routes, such as intravenous or oral administration, for both systemic and local drug delivery, and it is simple to administer. This technique is also painless. The goal of the dosage model for transdermal medications is to simultaneously enhance drug efflux from the skin into the systemic circulation while minimizing drug metabolism and retention in the skin. The selected drug for the present formulation is Allopurinol, a xanthine oxidase inhibitor that lowers uric acid levels in the body. Methodology: The goal of this study is the development of a matrix-type transdermal system of allopurinol with two different hydrophilic polymers, polyethylene glycol-4000(PEG-4000) and hydroxyl propyl methyl cellulose (HPMC), along with a hydrophobic polymer, Ethyl cellulose (EC), in different ratios by using the solvent evaporation technique to create a suitable matrix-type patch. Results and Discussion: The physicochemical characterization of thickness, folding endurance, moisture content, and drug-polymer compatibility has been studied. The drug release studies from the formulation, P1F3, showed maximum release of allopurinol (59.43%) in 5 h, where EC: PEG-4000 was 2:1; whereas P2F3 showed maximum release of allopurinol (57.28%) in 5 hours, where EC: HPMC was 2:1. In both cases, the release rate is retarding by increasing the proportion of hydrophobic polymer EC. Conclusion: The physicochemical evaluation of the prepared transdermal patches revealed good physical stability, with controlled drug release achieved by varying the ratios of hydrophilic and hydrophobic polymers.

Formulation and characterization of spray-dried clarithromycin microparticles with improved dissolution and potential for oral bioavailability

2026-01-17T06:39:34+00:00

Background: Clarithromycin, a macrolide antibiotic, exhibits limited aqueous solubility, which restricts its dissolution and bioavailability. Enhancing its solubility through novel formulation strategies is essential to improve therapeutic efficacy. Spray drying with hydrophilic carriers is an effective approach for drug particle engineering to improve dissolution. Methodology: Clarithromycin microparticles were prepared by the spray drying technique using hydroxypropyl-β-cyclodextrin (HP-β-CD) and Kollicoat IR® as hydrophilic polymers. The formulations were prepared in different drug-to-polymer ratios. Physicochemical characterization was performed using differential scanning calorimetry (DSC) and powder X-ray diffractometry (XRD) to study the crystalline-to-amorphous transition. Scanning electron microscopy (SEM) was used to assess particle morphology. Dissolution studies were carried out and compared with the pure drug, physical mixtures, and marketed clarithromycin tablets. Results and Discussion: DSC and XRD analyses confirmed the transformation of clarithromycin from a crystalline to an amorphous state within the spray-dried microparticles. SEM images revealed uniform spherical particles with porous surfaces. The optimized spray-dried formulation (CH 1:1) achieved 85.42 ± 0.47% drug release within 10 min and 96.28 ± 1.13% at 60 min, compared to 57.54 ± 1.54% and 81.54 ± 1.87%, respectively, for the marketed tablet. This corresponds to an approximately 1.5-fold enhancement in early dissolution. Conclusion: Spray drying with HP-β-CD and Kollicoat IR® successfully enhanced the solubility and dissolution of clarithromycin. The approach demonstrates potential to develop effective immediate-release tablets, with markedly improved in-vitro dissolution compared with the marketed product, indicating potential for enhanced oral bioavailability.

Formulation and evaluation of piperacillin tazobactam loaded aquasomal gel for the treatment of noma

2026-01-20T05:45:25+00:00

Background: Noma is a rapidly progressing gangrenous disease that affects the oral and facial tissues, mainly in malnourished and immunocompromised children. Delayed intervention often results in severe tissue destruction, facial deformity, and high morbidity. Although broad-spectrum antibiotics are routinely employed, conventional dosage forms often fail to achieve sufficient drug concentrations at the site of infection. Poor local absorption, limited tissue penetration, and the need for repeated administration reduce therapeutic effectiveness and patient compliance. Hence, a novel topical drug delivery system is required to enhance local drug delivery and clinical outcomes. This manuscript aims to formulate and evaluate a Piperacillin–Tazobactam-loaded Aquasomal gel for topical treatment of Noma. Methodology: Aquasomes composed of a calcium phosphate core coated with trehalose were prepared by the sonication method for topical delivery of Piperacillin–Tazobactam. A Central Composite Design (CCD) using Design-Expert® software was used to optimize formulation variables to improve entrapment efficiency and control drug release. The optimized Aquasomes were evaluated for particle size, polydispersity index, zeta potential, and drug entrapment efficiency, and then incorporated into a 1% Carbopol gel. Results & Discussion: The optimized formulation exhibited a particle size of 186 nm, a zeta potential of –19.37 mV, an entrapment efficiency of 68.18%, and sustained drug release of 61.1%. The gel exhibited suitable physicochemical properties and strong antibacterial activity against methicillin-resistant Staphylococcus aureus. Conclusion: The developed Aquasomal gel represents a promising topical therapy for the effective management of Noma.

Development and optimization of zingerone-loaded PLGA oil-based nanocarriers for enhanced solubility and sustained drug release

2026-01-23T04:14:47+00:00

Background: Zingerone, a phenolic constituent of Zingiber officinale, possesses notable antioxidant, anti-inflammatory, and anticancer activities. Its therapeutic use is limited by poor water solubility and low oral bioavailability, resulting in suboptimal efficacy. Polymeric nanocarriers, especially poly(lactic-co-glycolic acid) (PLGA)-based systems, offer an effective approach to enhance solubility, stability, and controlled drug delivery. Integration of lipid components into PLGA matrices can further improve drug loading and solubilization. This study focused on the design and optimization of zingerone-loaded PLGA oil-based nanocarriers to improve solubility and sustained release. Methodology: Solubility screening of zingerone in different oils identified peanut oil as the most suitable vehicle (54.31 mg/ml). Nanocarriers were prepared using a solvent evaporation method, producing nine formulations (F1–F9) with varying oil content and homogenization speeds. Characterization included particle size and zeta potential analysis, FTIR, DSC, SEM, and drug content determination using UV spectroscopy and HPLC. Drug release was studied using a dialysis membrane in phosphate buffer (pH 6.4), and stability testing was performed for the optimized formulation. Results and Discussion: The optimized batch (F4) exhibited a particle size of 79.7 nm, a zeta potential of −27.3 mV, and a drug content of 99.73%. Solubility increased more than 30-fold (5.44 mg/ml), with sustained drug release reaching 97.7% over 24 hours. Characterization confirmed efficient encapsulation and formulation stability. Conclusion: PLGA oil-based nanocarriers significantly improved zingerone solubility and enabled controlled release, indicating strong potential for further pharmacokinetic and therapeutic evaluation.

Design and evaluation of sustained-release vildagliptin tablets using natural plant mucilages as functional polymers

2026-02-16T06:55:02+00:00

Background: Natural plant-derived mucilages are gaining attention as biodegradable and biocompatible alternatives to synthetic polymers in sustained-release drug delivery systems. This study focuses on the development of prolonged-release matrix tablets of Vildagliptin using mucilages from Mimosa pudica seeds and Tinospora sinensis stems for improved glycemic control in type II diabetes mellitus. Methodology: Mucilages were extracted by aqueous extraction and evaluated for physicochemical properties. The swelling index ranged from 250–280%, with a near-neutral pH (6.5–7.0). Matrix tablets were prepared by direct compression and assessed for hardness (5.2–6.1 kg/cm²), friability (<1%), weight variation, and drug content (98.2–101.4%). In vitro drug release studies were conducted for 12 hours. Drug–polymer compatibility was analyzed using FTIR spectroscopy, and release kinetics were evaluated using mathematical models. Results and Discussion: FTIR analysis confirmed the absence of drug–polymer interactions. The optimized formulation showed 96.8% cumulative drug release over 12 hours, indicating effective sustained-release performance. The release followed the Korsmeyer–Peppas model (R² = 0.97) with anomalous (non-Fickian) transport, suggesting a combination of diffusion and polymer erosion mechanisms. The combination of the two mucilages demonstrated superior release control compared to either polymer alone. Conclusion: Mimosa pudica and Tinospora sinensis mucilages exhibit strong potential as natural matrix-forming agents for sustained-release formulations of Vildagliptin, providing a sustainable, cost-effective alternative to synthetic polymers.

Biochemical characterization, GC-MS metabolite profiling, and heavy metals assessment of Rokshi: safety assessment and nutritional potential of a traditional fermented rice beverage of Monpa tribe

2026-02-18T07:29:36+00:00

Background: Rokshi is a traditional fermented rice beverage widely consumed by the Monpa tribe of Arunachal Pradesh, a Northeastern State in India, with cultural, nutritional, and biochemical significance. Methodology: Standard analytical methods were employed to determine pH, alcohol content, total acidity, viscosity, and antioxidant properties. Microbial count was assessed using the plate count method. Metabolite profiling and heavy metals analysis were conducted using GC-MS and ICP-OES, respectively. Results and Discussion: Rokshi were reported to be acidic and rich in metabolically important compounds. One-month-old Rokshi beverage showed increased alcohol content (7.54% v/v) as compared to fresh Rokshi beverage (2.59% v/v), with a pH of 4.10 (fresh), which decreased to 3.09 during storage. Total acidity increased from 0.58% to 0.78% after one month of storage. Total flavonoid and phenolic content were 0.205 mg QE/mL and 0.928 mg GAE/mL, respectively, with moderate antioxidant activity. Microbial load decreased in the starter culture (2.15 log CFU/mL) to 0.55 log CFU/mL in the final product. GC-MS analysis identified 28 metabolites, predominantly amino acids, sugars, organic acids, and alcohol. Heavy metals (Cd, Pb, Cr, Mn, Fe, Zn, Ni) were also detected, within the maximum permissible limit, and TTHQ values (<1) indicated no significant non-carcinogenic risk at 250 mL/day consumption. Conclusion: The current study showed that Rokshi holds promise for its nutritional and biochemical properties and has moderate antioxidant potential. The presence of a few biogenic amines and trace contaminants emphasizes the need for purification and further toxicological validation to ensure consumer safety and promote nutraceutical applications for commercial use as a functional fermented beverage.

Development and evaluation of a Cassia tora-based herbal antacid suspension

2026-02-06T05:42:24+00:00

Background: Synthetic antacids are frequently used to manage gastric hyperacidity; however, their potential for long-term adverse effects has catalyzed significant interest in developing safer herbal-based therapeutic alternatives. Cassia tora, traditionally used for gastrointestinal disorders, contains gastroprotective flavonoids, anthraquinones, and tannins. Methodology: To develop and evaluate a Cassia tora-based herbal antacid suspension, assessing its physicochemical stability, microbial safety, phytochemical profile, and acid-neutralizing capacity against a marketed antacid. A methanolic Cassia tora extract was formulated into a suspension with aluminium hydroxide, magnesium hydroxide, and magnesium trisilicate, using controlled flocculation and a structured vehicle. The evaluations included physicochemical properties (pH, viscosity, redispersibility), microbial safety, phytochemical screening, and a 90-day accelerated stability study (ICH guidelines). The acid-neutralizing capacity (ANC) was determined via back titration and compared to that of the marketed antacid and the control. Results and Discussion: The suspension demonstrated acceptable stability over 90 days, with minimal changes in pH (8.86→8.82) and viscosity (1780→1738 cP), and retained easy redispersibility. The microbial counts remained within the pharmacopeial limits. Phytochemical screening confirmed the presence of flavonoids, tannins, and saponins. The ANC was 1.68 mEq, comparable to that of a marketed antacid (2.15 mEq) and significantly superior to that of the control (0.02 mEq). Conclusion: A stable, efficacious Cassia tora-based herbal antacid suspension was successfully developed, exhibiting physicochemical stability, microbial safety, and an ANC comparable to that of commercial formulations. This supports its potential as a natural adjunct, though further in vivo and clinical studies are needed to confirm therapeutic applicability.