Journal of Applied Pharmaceutical Research

A review on the structure, distribution, and biological activities of biflavonoids in clusiaceae

Anjana Unni — 2025-10-31

Background: The Clusiaceae family is widely distributed in tropical and subtropical climates, with a rich source of structurally diverse metabolites. Among these, biflavonoids stand out due to their complex structures and significant pharmacological activities. This review aims to examine data on various Clusiacean biflavonoids, their structural diversity, and bioactivity, thereby increasing the understanding of their implications in both traditional and modern medicine. Methodology: Data were collected from electronic databases like PubMed, Elsevier, Springer, and Google Scholar. The structural categorization of biflavonoids was based on the nature of linkage and substituent variations that influence their biological activities. Their distribution across Clusiacean members further highlights their chemotaxonomic importance. Additionally, structure-activity relationship studies reveal that specific linkages and functional groups enhance biological activity. Results and Discussion: Studies indicate that Clusiacean biflavonoids are potential candidates for drug discovery and therapeutic development due to their varied pharmacological activities. Approximately 21 biflavonoids from Clusiacean members are included in this review; nine of them exhibit antioxidant, five antimicrobial, five early antigen inhibition, four monoamine oxidase inhibition, three anti-inflammatory, three neuromuscular transmission inhibition, one antidiabetic, one anti-aging, and one hypocholesterolemic activity. Conclusion: Clusiacean biflavonoids possess desirable compounds for drug development owing to their diverse pharmacological activities, including antiviral, anti-inflammatory, anti-cancer, antioxidant, and neuroprotective properties, and so on. Overall, this article analyzes different biflavonoids obtained from Clusiaceae species, focusing on their structural diversity, biological importance, and structure-activity relationships.

Heterocyclic scaffolds in antibiofilm strategies against drug-resistant pathogens: a comprehensive review

Tamalika Chakraborty — 2025-10-31

Background: Antimicrobial resistance (AMR) is a primary global health concern, exacerbated by the ability of drug-resistant pathogens to form biofilms. These biofilms, which harbor microbial communities embedded in an extracellular polymeric matrix (EPS), enhance antibiotic resistance and immune responses, leading to persistent infections. Heterocyclic compounds have shown significant potential in combating biofilm-associated infections due to their structural diversity and mechanisms of action. Methodology: This review systematically examines the antibiofilm potential of various heterocyclic scaffolds, including imidazoles, pyrazoles, indoles, quinolines, coumarins, and select six-membered heterocycles (pyridine, morpholine, piperazine). Studies were analyzed based on their mechanisms of action, structure-activity relationships (SAR), and synergy with conventional antibiotics. Result and Discussion: Imidazole derivatives disrupted biofilm integrity and enhanced antibiotic susceptibility in Pseudomonas aeruginosa and Staphylococcus aureus, with IC₅₀ values ranging from 0.53 to 9.5 µM. Pyrazole-based compounds inhibited Staphylococcus epidermidis biofilms, with IC50 values ranging from 3.1 to 15.6 µg/mL. Indole derivatives, particularly pyrroloindoline triazole amides, inhibited MRSA biofilms with IC₅₀ values as low as 2.8 µM by targeting quorum sensing and curli production. Quinoline compounds demonstrated greater than 90% inhibition of E. coli and P. aeruginosa biofilms and showed synergistic effects with antibiotics. Conclusion: Heterocyclic compounds exhibit promising antibiofilm activity, presenting a viable approach to overcoming AMR. These compounds not only disrupt biofilm formation but also enhance the efficacy of conventional antibiotics through synergistic interactions. Such synergy potentiates the antimicrobial effect by improving antibiotic penetration or disrupting resistance pathways. Future research should focus on optimizing pharmacokinetics and exploring these synergistic combinations to improve clinical applicability.

Assessment of pharmacognostical, physiochemical, and in-vitro anti-inflammatory potential of S. cordata

Devendra Kumar Sahu — 2025-10-31

Background: The current study aimed to investigate the pharmacognostical, physiochemical, and anti-inflammatory potential of Sida cordata. In this study, macroscopic, microscopic, and physicochemical analyses were performed. Methodology: This medicinal plant, commonly used in traditional medicine, was evaluated using the in vitro albumin denaturation method. The study aimed to assess the plant's ability to inhibit protein denaturation, a critical factor in the inflammatory process. The water extract and acetic acid extract of Sida cordata were tested at various concentrations (10, 50, 100, 150, 200, 250 µg/ml), and the results indicated a dose-dependent inhibition of albumin denaturation. Result & Discussion: The rate of inhibition of egg albumin denaturation for water extract (WE) is 86.55±0.63, and acetic acid extract (AAE) is 82.18±1.43. The maximum inhibition observed was compared with the standard anti-inflammatory drug (diclofenac sodium). Conclusion: These findings suggest that the water and acetic acid extracts of Sida cordata possess significant anti-inflammatory activity, supporting its traditional use as a remedy for inflammatory conditions.

Design, formulation, and evaluation of hydrogel network based microbeads for prolonged release of valacyclovir

Sankar Narayan Bhunia — 2025-10-31

Background: This study aimed to formulate and develop hydrogel network-based microbeads for the prolonged release of the antiviral drug Valacyclovir, focusing on the effect of natural gum/polymer ratios in their preparation. Methodology: Microbeads containing Valacyclovir hydrochloride were prepared using the ionotropic gelation method, which involved sodium alginate and gellan gum as the polymers, and aluminum chloride as the crosslinking agent. Result: In the evaluation, the F1 batch exhibited the highest swelling capacity, drug entrapment efficiency, and drug release profile. Across all formulations, the particles were round to oval in shape, with sizes ranging from 598 to 816µm. Drug release kinetics revealed that the Higuchi model best explained the formulations. The surface morphology of the best-performing formulation was examined using scanning electron microscopy (SEM). Discussion: The findings proposed that the prepared microbeads function as swellable matrix-type systems, enabling prolonged drug delivery. The Higuchi model fit supported a diffusion-controlled release mechanism, while the SEM analysis confirmed the suitability of the microbead structure for sustained release applications. Conclusion: These kinds of ionotropically-gelled alginate-based microbeads may improve patient compliance by reducing dosing frequency and enhancing oral bioavailability.

Optimization of green LC-MS method for rosuvastatin and teneligliptin using AQbD chemometric approach

S R Aswathy — 2025-10-31

Background: Rosuvastatin combined with Teneligliptin formulation is commonly used in the treatment of Diabetic dyslipidaemia. However, only a few analytical methods have been published for the examination of this drug in a synthetic mixture or in a pharmaceutical dosage form. This study demonstrates the successful application of AQbD principles in developing a reliable, efficient, and environmentally friendly LC-MS method. Methodology: Box-Behnken Model: Design of experiment (DoE) strategy to identify and optimize critical method parameters using systematic risk assessment. Methanol: 10mM potassium dihydrogen orthophosphate [pH:6.0] (35:65v/v) was the mobile phase employed in the final optimized LC method, and this was using a Waters LC Xbridge C18 Column 5µm (4.6x250mm) as the stationary phase. The experiment was conducted at a flow rate of 1 mL/min, with a 10 µL injection volume, and an ESI-MS-QDA Detector for detection. An analytical method for validation was applied in accordance with ICH Q2 (R1) guidelines. Results and Discussion: The retention times of Rosuvastatin and Teneligliptin were observed at 4.392 and 3.202 minutes, respectively. The optimized technique showed excellent linearity, accuracy, precision, and robustness. Additionally, AGREE metrics and AES were used for assessing the eco-friendly nature of the developed method. Conclusion: The combination of green principles with AQbD experimental design ensures the robustness of the method. This combined framework is used for the first time in method development for the analysis of rosuvastatin with teneligliptin in formulations. Based on the above facts, an economical, robust, and time-saving method has been developed for assessing the quality control of rosuvastatin with teneligliptin in both pharmaceutical and pure forms.

Phytochemical screening, antioxidant activity and GC-MS analysis of Syzygium diospyrifolium (Wall.Ex Duthie) S.N. Mitra: A medicinal plant from Meghalaya, India

Amaryllis Langbang — 2025-10-31

Background: Syzygium diospyrifolium (Wall.ex Duthie) S.N. Mitra is a traditionally valued but underexplored medicinal plant from Meghalaya, India. This study aimed to assess the phytochemical composition, antioxidant potential, and GC–MS profile of its fruit and leaf extracts to explore their therapeutic prospects. Methods: Methanol and ethanol extracts of the fruits and leaves were prepared using a Soxhlet extraction apparatus. Percentage yields were determined, and qualitative phytochemical screening identified secondary metabolites. Total phenolic content (TPC) and total flavonoid content (TFC) were quantified spectrophotometrically, while antioxidant activity was evaluated using DPPH radical scavenging and reducing power assays. GC–MS analysis identified bioactive compounds. All experiments were performed in triplicate (n=3), and results were expressed as mean ± SD with significance at p < 0.05 (Student’s t-test). Results: Methanol extracts yielded higher percentages (fruit: 15.2% w/w; leaf: 14.4% w/w) than ethanol extracts. Both extracts contained alkaloids, glycosides, saponins, phenols, tannins, flavonoids, proteins, amino acids, and diterpenes. Fruits exhibited higher TPC (52.23 mg GAE/g) and TFC (152 mg QE/g) than leaves (26.96 mg GAE/g; 96.86 mg QE/g; p < 0.05). Antioxidant assays showed stronger activity in fruits (DPPH IC₅₀: 133.95 µg/mL) than leaves (215.11 µg/mL). GC–MS analysis identified sugars, fatty acid amides, sterols, terpenoids, and phenolic derivatives, including DL-Arabinose, D-Allose, and 13-Docosenamide (Z), reported for the first time. Conclusion: This first GC-MS-based phytochemical profiling of S. diospyrifolium (Wall.ex Duthie) S.N. Mitra reveals its fruits as rich in phenolic and flavonoid compounds with significant antioxidant potential, supporting its promise for nutraceutical and phytopharmaceutical applications

Design and optimization of chitosan microspheres loaded with green tea phytosomes for sustained release

Juti Rani Devi — 2025-10-31

Background: Phytosomes are nanovesicular systems that integrate plant extracts with phospholipids to improve the solubility, stability, and bioavailability of phytoconstituents. Green tea (Camellia sinensis) is rich in polyphenols such as epigallocatechin gallate (EGCG) and epigallocatechin (EGC), which possess significant therapeutic potential but are limited by poor absorption and stability. The present study aimed to formulate and evaluate green tea extract–loaded phytosome-incorporated microspheres with desirable physicochemical characteristics for sustained delivery. Methodology: Phytosomes were prepared using the thin-layer hydration method with varying molar ratios (0.5–1.0) of phospholipids to standardized green tea extract (sample 1 and sample 2). The optimized phytosomes were further encapsulated into microspheres via emulsion cross-linking, employing different concentrations of glutaraldehyde and polymer to obtain nine formulations. Design Expert software was applied for optimization, and the microspheres were evaluated for micrometric properties, entrapment efficiency, drug loading, drug release, swelling behaviour, mucoadhesion, stability, and surface morphology. Results and Discussion: The prepared microspheres exhibited a spherical morphology with satisfactory physicochemical properties. Among the formulations, batch F3 of sample 1 demonstrated the most promising results, achieving 87% yield, 77% drug entrapment efficiency, 30% drug loading, and 91.87% cumulative drug release up to 9 hours, along with favorable swelling and mucoadhesion properties. Stability studies further confirmed the reliability of the formulation. Conclusion: Overall, the developed phytosome-loaded microspheres of green tea extract exhibited an improved release profile, stability, and potential fwr sustained drug delivery, suggesting their applicability in enhancing the therapeutic efficacy of green tea polyphenols.

Design and optimization of folate-targeted lipid-polymer hybrid nanoparticles co-encapsulating dexamethasone and curcumin for synergistic anti-inflammatory efficacy in rheumatoid arthritis

Ekta Panchal — 2025-10-31

Background: Rheumatoid Arthritis (RA) is a chronic immune-mediated disorder characterized by synovial inflammation and joint destruction. Current therapies are limited by systemic toxicity and poor bioavailability. This research developed Dexamethasone (Dex) and Curcumin (Cur) loaded Folate Lipid Polymer Hybrid Nanoparticles (DCFLPs) to achieve synergistic anti-inflammatory action for RA. Methodology: DCFLPs were synthesized by the ionic gelation technique. Furthermore, Box-Behnken Design (BBD) formulations were optimized and evaluated for size distribution, PDI, ζ potential, structural features, % encapsulation efficiency (EE), in vitro release profile, and cell line studies using RAW 264.7 cells. Results and Discussion: Optimized DCFLPs revealed an average particle size of 287.8 ± 1.32 nm and PDI 0.25 with positive ζ potential 5.4 mV, and have shown high entrapment efficiencies for Dex (89.12 ± 0.087%) and Cur (98.27± 0.110%). Cytotoxicity assays showed superior anti-inflammatory activity, and enhanced cellular uptake was observed in cell line studies. Conclusion: DCFLPs offer an auspicious approach for targeted RA therapy by combining controlled drug release, reduced systemic toxicity, and enhanced site-specific delivery. These findings suggest that the synthesized formulation has the potential to serve as a viable approach for in vivo translation, future preclinical evaluation, and effective progression towards clinical application in RA management.

Formulation and optimization of metformin-berberine loaded solid lipid nanoparticles for their neuroprotective effects in the brain

Ravina Yadav — 2025-10-31

Background: The increasing prevalence of Type 2 Diabetes Mellitus (T2DM) is associated with a heightened risk of developing Alzheimer’s Disease (AD), highlighting the need for effective therapeutic strategies that address the shared pathophysiological mechanisms in both conditions. Methodology: The Metformin-Berberine loaded solid lipid particles (MBSLNs) were prepared by dispersion of different concentrations of stearic acid, polysorbate 80, poloxamer 407, sesame oil, metformin, and berberine. Factor screening studies have been done to identify the influential components. An optimization study was then conducted using a three-factor Box-Behnken design with Design-Expert software. In-Vivo studies confirmed the neuroprotective role of SLNs. Results: The optimized concentrations of the variable factors were determined using the overlay plot generated by the software, resulting in stearic acid (4.84%), polysorbate 80 (1.50%), Poloxamer 407 (1%), and sesame oil (0.31%). The responses, particle size (10–200 nm), zeta potential (> ±30 mV), and polydispersity index (PDI) (0–1) were achieved within the desired range. Discussion: The closeness in experimental and predicted values confirms the reliability of the optimization technique. The optimized formulation exhibits a significant reduction in oxidative stress, and decreased glucose levels were observed when compared to the control, indicating a neuroprotective effect of the formulation. Conclusion: The optimized MBSLNs were affected by the independent parameters examined, including stearic acid, polysorbate 80, Poloxamer 407, and sesame oil concentrations, with significant effects on particle size, zeta potential, and size distribution. The utilization of MBSLNs has emerged as a remarkably effective strategy for enhancing the biological activity of Metformin and berberine in treating T2DM-induced AD.

Development and evaluation of non-saccharide polymer-based taste-masked clarithromycin tablets: a novel approach to improve pediatric compliance

Mahesh Bhalsing — 2025-10-31

Background: Clarithromycin, a macrolide antibiotic, is commonly prescribed for respiratory and skin infections. However, its intensely bitter taste significantly hampers patient compliance, especially in pediatric and geriatric populations. The present study focused on formulating a novel taste-masked clarithromycin tablet using non-saccharide polymers to improve palatability while maintaining pharmacological performance. Methodology: Taste masking was accomplished by employing Eudragit E-100, Ethyl Cellulose, and Hydroxypropyl-β-Cyclodextrin (HP-β-CD) as coating agents. Granules were formulated using a bottom-spray fluidized bed coating process, followed by compression into tablets. These were assessed for physical parameters, disintegration time, in vitro drug release, and sensory evaluation using an electronic tongue system. The dissolution behavior was compared with that of a marketed clarithromycin formulation. Stability testing was conducted under accelerated (40°C/75% RH) and long-term (25°C/60% RH) storage conditions. Result and Discussion: The optimized formulation (Batch B9) demonstrated complete taste masking, exhibiting a bitterness score of 0 on the electronic tongue. Sensory data projected an over 85% improvement in patient acceptability. The tablets disintegrated within 60 seconds and showed a drug release of 98.1% within 30 minutes. Comparative dissolution profiling indicated no statistically significant difference (p > 0.05) between the test and reference products. Stability studies confirmed robust physicochemical stability for six months under both storage conditions. Conclusion: The study successfully developed a taste-masked clarithromycin tablet employing non-saccharide polymers, ensuring effective taste masking, rapid disintegration, and consistent drug release. This formulation offers a promising approach to enhance treatment compliance, particularly in populations sensitive to taste.

Biogenic zinc oxide nanoparticles from Saraca asoca: cytotoxicity, antioxidant, antimicrobial evaluation, and topical gel development

Aishwarya Jain — 2025-10-31

Background: Green synthesis of nanoparticles offers an eco-friendly and cost-effective alternative to conventional methods. Saraca asoca, a traditionally valued medicinal plant, contains bioactive compounds suitable for the fabrication of nanoparticles. This study reports the synthesis of zinc oxide nanoparticles (ZnO NPs) using Saraca asoca bark apozem and their incorporation into a biocompatible chitosan gel for topical applications. Methodology: ZnO NPs were synthesized via a green route using varying concentrations of zinc acetate (0.05–0.15 M) and Saraca asoca bark apozem (75–150 mg/mL), optimized through a 3² factorial design. The nanoparticles exhibited favorable formulation efficiency with % yield (40–46%), entrapment efficiency (55–62%), and drug loading (35–40%). Characterization confirmed nanoscale size (72.7–134.8 nm), negative zeta potential (–38.2 to –50.4 mV), UV–Vis absorbance (λmax = 366 nm), FTIR peaks of stabilizing –OH and –COO⁻ groups, and crystalline PXRD patterns. The optimized nanoparticles were incorporated into a 2% chitosan gel (Ash–ZnO NPs Cs gel). Results and Discussion: Antioxidant studies revealed strong free radical scavenging potential (IC₅₀ = 19.8 µg/mL). The Ash–ZnO NPs exhibited antimicrobial activity against Staphylococcus aureus and Candida albicans (MICs: 156.25 and 78.12 µg/mL). Cytotoxicity studies confirmed negligible toxicity (LC₅₀ > 1000 µg/mL). In vitro release studies demonstrated sustained and diffusion-controlled drug release, with Ash–ZnO NPs Cs gel achieving 96% release at 48 h compared to the burst release of silver nitrate gel. Conclusion: Saraca asoca-mediated ZnO NPs incorporated in chitosan gel represent a safe, stable, and multifunctional topical formulation. Their strong antioxidant, antimicrobial, biocompatible, and sustained release properties underscore their potential for wound healing and skin infection management.

Evaluation of a polyherbal formulation in gastric ulcer models induced by naproxen and acetic acid in Wistar Rats

Kiran Niuratti Khodake — 2025-10-31

Background: Gastric ulcers remain a prevalent gastrointestinal disorder, often exacerbated by non-steroidal anti-inflammatory drugs (NSAIDs) like Naproxen and irritants such as acetic acid. The investigation focuses on evaluating the gastroprotective properties of a formulation composed of standardized extracts from traditionally used medicinal plants, evaluated in Wistar rat models with experimentally induced gastric ulcers. Methodology: Ulcers were induced using Naproxen (NSAID-induced model) and acetic acid (chronic ulcer model) to mimic acute and chronic ulcerative conditions. The polyherbal formulation was administered orally at graded doses prior to ulcer induction. Ulcer index, gastric volume, pH, and histopathological parameters were assessed to determine protective effects. Results: The polyherbal formulation significantly reduced ulcer index in a dose-dependent manner, with the highest dose (1180 mg/kg) lowering the index to 0.44 ± 0.02 in Naproxen-induced ulcers (67.45% protection) and to 2.21 ± 0.01 in acetic acid-induced ulcers (61.25% protection), closely approaching omeprazole’s efficacy. Discussion: The formulation demonstrated a significant reduction in ulcer index and improved gastric mucosal integrity, with notable restoration of antioxidant defense mechanisms. Histological studies revealed reduced mucosal damage and inflammation compared to control groups. Conclusion: These outcomes recommend that the polyherbal formulation utilizes a protective effect against gastric ulcers, likely through cytoprotective, anti-inflammatory, and antioxidant mechanisms. The study supports the therapeutic potential of polyherbal combinations in managing gastric ulcers and encourages further clinical investigation.

Optimization of fast melting olanzapine tablets using solid dispersion and response surface methodology

Sundaramoorthi Revathi — 2025-10-31

Background: Olanzapine is a poorly water-soluble, anti-psychotic drug that belongs to the class of thiobenzodiazepines, which has a bioavailability of 60 – 65%. The purpose of this research work is to enhance the solubility of olanzapine by the solid dispersion technique using different water-soluble carriers, using a phase solubility study using a 2⁴ factorial design, and to incorporate the solid dispersion of olanzapine to formulate fast-melting tablets using different superdisintegrants. Methodology: The fast-melting tablets were prepared using the wet granulation technique and optimized through a 2³ full factorial design. The independent variables are sodium starch glycolate (X1), sodium carboxymethyl cellulose (X2), and the method of preparation of the solid dispersion (X3). The dependent variables are hardness (Y1), friability (Y2), disintegration time (Y3), and in vitro drug release studies (Y4). The kinship between independent and dependent variables was demonstrated using contour diagrams. Additionally, the prepared fast-melting tablets were analysed for their weight variation, drug content uniformity, and other dependent variables. Results and Discussion: The fast-melting tablets (batch F6) were considered desirable based on their drug content (99.5% & drug release of 99.3% in 20 minutes, following first–order and Higuchi kinetics. The difference factor f1and f2 similarity factor were found to be 2.43% and 83%, respectively, for the optimized formulation FM2, and the drug release was greater than that of the marketed product. Conclusion: It is evident that the optimized formulation FM2 appears to be a promising system that facilitates the rapid release of olanzapine compared to other formulations.

QbD-guided HPTLC method development and validation for quantitative estimation of anticancer drugs

Bhavik Jani — 2025-10-31

Background: Olaparib, Abiraterone acetate, and Pazopanib are critical anticancer agents used in the treatment of breast/ovarian, prostate, and renal cancers, respectively. Ensuring their quality through precise, cost-effective analytical techniques is vital for routine quality control (QC). Given their clinical importance, a robust method capable of quantifying these drugs individually and indicating their stability under stress is highly desirable. Methodology: High-performance thin-layer chromatography (HPTLC) methods were developed for each drug, guided by a Quality by Design (QbD) approach. A 2³ factorial design was employed to optimize three critical method parameters: mobile phase composition, chamber saturation time, and detection wavelength. Chromatographic analysis was performed on aluminum-backed silica gel plates with detection wavelengths set at 278 nm (Olaparib), 255 nm (Abiraterone acetate), and 254 nm (Pazopanib). Method validation followed ICH Q2(R2) guidelines, assessing linearity, accuracy, precision, LOD/LOQ, specificity, and robustness. Forced degradation under acidic, basic, oxidative, thermal, and photolytic conditions was evaluated to assess the stability-indicating capability. Results and Discussion: All methods exhibited strong linearity (r² > 0.997), high accuracy (98–102% recovery), and precision (%RSD < 2). Sensitivity was excellent, with LOD as low as 28 ng/spot for Olaparib. Under stress, degradation ranged from 5% to 20%, with distinct degradant peaks and peak purity indices of> 0.995, confirming no co-elution and indicating stability. The validated methods were successfully applied to stressed marketed formulations. Conclusion: The QbD-optimized HPTLC methods are accurate, economical, and stability-indicating, making them suitable for routine QC of Olaparib, Abiraterone acetate, and Pazopanib in pharmaceutical dosage forms.

Formulation and evaluation of ethosomal gel containing Nyctanthes arbor-tristis leaf extract using design of experiments for enhanced topical delivery

Kamlesh Kumar Yadav — 2025-10-31

Background: Nyctanthes arbor-tristis (L.), generally known as Night Jasmine, is a medicinal plant renowned for its antimicrobial and antioxidant activities. Despite its traditional therapeutic use, there is limited scientific research on its detailed botanical characterization, phytochemical composition, and incorporation into advanced pharmaceutical formulations. This study aims to fill this gap by investigating the botanical and phytochemical profiles of N. arbor-tristis leaves and by developing optimized ethosomal gel formulations for enhanced topical drug delivery. Methodology: Comprehensive phytochemical screening revealed the existence of steroids, alkaloids, flavonoids, and tannins. Quality control parameters such as moisture content and ash values were evaluated. Ethosomal gels were prepared with phospholipids, cholesterol, and ethanol, and formulation optimization was performed using a Design of Experiments (DoE) approach. The developed formulations were systematically evaluated for particle size, polydispersity index, zeta potential, entrapment efficiency, and in vitro drug release profiles. Result and Discussion: Optimized formulations (EG-NAT-12 and EG-NAT-11) exhibited favorable nanoscale particle sizes (130.0 nm and 132.5 nm), low polydispersity indices (0.258 ± 0.027 and 0.274 ± 0.029), high negative zeta potentials (−23.5 mV to −24.0 mV), and high entrapment efficiencies (up to 89.8%). EG-NAT-12 demonstrated sustained drug release, with 84.0% released over 6 hrs. Stability testing confirmed the physical and chemical stability of the formulations over 45 days at both refrigerated and room temperatures. Conclusion: This study demonstrates the potential of Nyctanthes arbor-tristis ethosomal gels as effective topical drug delivery systems, integrating traditional herbal benefits with modern nanotechnology to enhance their efficacy.

Antimicrobial activity of bioactive compounds extracted from Chara globularis Thuill

M P Jeevitha — 2025-10-31

Background: The algae, a vastly diversified group of species on Earth, offer numerous benefits to humanity. Chara globularis is one such green alga that contains potential bioactive compounds. Methodology: This current study investigates the antifungal and antibacterial potential of Chara globularis extracts obtained using methanol, acetone, and hexane solvents, along with their phytochemical and medicinal profiles. Results & discussion: The antifungal activity was evaluated against clinically significant fungal strains, including Microsporum gypsum, Trichophyton rubrum, and T. mentagrophytes. The methanol extracts exhibited the most potent inhibition zones, with T. rubrum showing a maximum inhibition of 24 mm at a concentration of 4 mg. Also, antibacterial assays against pathogens such as Staphylococcus aureus, Escherichia coli, and Klebsiella pneumoniae demonstrated strong activity, especially in methanol and acetone extracts at higher concentrations. Comparative control studies using fluconazole and tetracycline confirmed the efficacy of the extracts, suggesting potential for pharmaceutical application. GC-MS analysis of the methanol extract identified 26 bioactive compounds, notably pentadecanoic acid and eicosatrienoic acid, which possess antimicrobial, anti-inflammatory, and cardioprotective properties. Conclusion: Nutrient profiling further revealed high levels of essential macro and micronutrients, highlighting the nutritional value of Chara globularis. The findings support the plant’s potential as a natural source of therapeutic agents with broad-spectrum antimicrobial and nutraceutical applications.

pH independent controlled release of verapamil hydrochloride using HPMC-alginate matrices & organic acids

R U Gaware — 2025-10-31

Background: Verapamil HCl, a weakly basic drug, exhibits pH-dependent solubility that limits sustained-release formulation efficacy. This study developed controlled-release matrix tablets using HPMC, sodium alginate, and organic acids to achieve pH-independent drug release. Methodology: Sixteen formulations (F1-F16) were prepared using a 2⁴ factorial design with varying concentrations of organic acids (citric/fumaric: 50-75 mg), sodium alginate (50-80 mg), and HPMC K4M (30-50 mg). Evaluations included pre- and post-compression studies, dissolution testing under a two-stage pH protocol (pH 1.2 for 2 hours, then pH 6.8 for 10 hours), microenvironmental pH monitoring, and kinetic modeling. Results and Discussion: All formulations met pharmaceutical standards, with hardness of 6.88-7.55 kg/cm², friability <0.55%, and drug content of 98.65-99.68%. Fumaric acid formulation F8 achieved superior performance with 89% drug release and the highest pH-independence (f₂ = 91.2) compared to control F1 (72% release, f₂ = 85.3). Microenvironmental pH monitoring revealed that F8 maintained sustained acidification (pH 4.10-4.75) for 12 hours, whereas citric acid formulations showed premature acid depletion. All formulations fitted the Korsmeyer-Peppas model (R² > 0.99), with F8 exhibiting diffusion-controlled release (n = 0.512). Statistical optimization identified fumaric acid as the most significant factor (F-value = 26.30, p = 0.0003). Conclusion: Incorporating 75 mg fumaric acid in HPMC-alginate matrices provides robust, pH-independent sustained release through maintained microenvironmental acidification, offering a validated solution for weakly basic drugs in sustained-release formulations.

Formulation and evaluation of moxifloxacin-loaded proniosomal gel for ocular delivery

Neha Kandpal — 2025-10-31

Background: The management of ocular disorders is particularly arduous due to the eye's distinctive anatomy. The cornea serves as a crucial obstacle to medication absorption, restricting the effectiveness of conventional dosage regimens. To address this issue, a proniosomal gel has been developed, comprising a lipid bilayer that emulates the corneal cell membrane, thereby enhancing drug transport across the cornea and resulting in improved bioavailability. Methodology: The Moxifloxacin-loaded Proniosomal gel was developed by the coacervation phase separation method. To determine the physicochemical characteristics of the gel, various evaluation parameters were conducted, including viscosity, pH, FTIR, zeta potential, polydispersity index (PDI), particle size (PS), entrapment efficacy (EE), SEM, and in vitro studies. Results and Discussion: The F5 optimized formulation exhibited a maximum EE of 94.47±0.23%, an ideal pH of 6.8, a PS of 105.4 nm, a PDI of 0.3678, and a zeta potential within ±30 mV. In-vitro drug release and kinetic studies showed that proniosomal gel followed first-order kinetic characteristics of drug released and a biphasic drug release pattern (There is an initial rapid release of the drug, followed by a slower, controlled release over an extended period). Conclusion: Proniosomal gels as drug delivery carriers increased corneal contact, penetration, and retention time in the eye, resulting in sustained action and increased bioavailability.

Phytochemical profiling and in silico evaluation of Brassica oleracea stem bioactives as novel aldose reductase inhibitors for diabetic neuropathy treatment

Rajashree Dadasaheb Ghogare — 2025-10-31

Background: Diabetic neuropathy affects over 50% of diabetic patients, causing significant morbidity and economic burden exceeding $327 billion annually. Current treatments offer limited relief, accompanied by considerable side effects. Aldose reductase inhibition represents a promising therapeutic approach, yet synthetic inhibitors face clinical challenges, including hepatotoxicity and inadequate safety margins. This study investigates Brassica oleracea stem bioactives as novel aldose reductase inhibitors. Methodology: Sequential extraction of Brassica oleracea stems employed ethanol and acetone solvents. Phytochemical screening utilized standard chemical tests, while HR-LCMS enabled metabolite identification. Molecular docking against human aldose reductase (PDB: 1US0) was performed using GeinDock Suite. Drug-likeness and ADME properties were assessed using SwissADME, in accordance with Lipinski's Rule of Five. Comprehensive pharmacokinetic parameters were also evaluated. Results and Discussion: HR-LCMS identified 33 bioactive compounds with identification scores >90%. Four lead compounds demonstrated optimal aldose reductase inhibitory potential with superior drug-likeness: Indole-3-acetonitrile (-8.9 kcal/mol, Ki=0.30 μM) approached reference inhibitors epalrestat (-9.9 kcal/mol) and sorbinil (-9.4 kcal/mol) with zero Lipinski violations. 18-Oxooleate (-7.5 kcal/mol) and Salicylamide (-7.6 kcal/mol) exhibited exceptional bioavailability (0.85) with minimal CYP450 inhibition. Phytosphingosine (-6.7 kcal/mol) displayed advantageous peripheral selectivity. Conclusion: Four B. oleracea compounds demonstrate optimal convergence of aldose reductase inhibitory potential and pharmaceutical feasibility, offering promising orally bioavailable candidates for diabetic neuropathy management. Their natural origin and favorable ADME profiles warrant immediate progression to in vitro validation and in vivo studies.

Development and validation of a robust QbD-guided (RP-HPLC) analytical technique for quantifying coenzyme Q10 in pharmaceutical dosage form

Vishal Kumar Pathak — 2025-10-31

Background: Coenzyme Q10 (CoQ10) is a lipophilic antioxidant that contributes to mitochondrial energy production but poses analytical challenges due to low solubility and oxidative sensitivity. An accurate and validated method is essential to ensure quality control of its pharmaceutical dosage forms. Methodology: A reverse-phase high-performance liquid chromatography (RP-HPLC) method was designed using Quality by Design (QbD) principles. A Central Composite Design was employed to study the influence of critical parameters, including flow rate, gradient time, and mobile phase ratio. Separation was carried out on a Gemini C18 column (250 × 4.6 mm, 5 µm) with gradient elution using ethyl acetate: acetonitrile (50:50) and methanol: acetonitrile (80:20) containing 0.1% ammonia. The method was validated in accordance with ICH-Q2 (R1) guidelines. Results: The optimized conditions yielded a sharp CoQ10 peak at approximately 12.9 minutes with high resolution (Rs > 36), theoretical plates (~33,800), and acceptable tailing (≤1.3). Linearity was established over 2.5–200 µg/mL (r² = 0.9997). Accuracy ranged from 99.2–101.4%, precision was within %RSD ≤1.5%, and robustness was demonstrated under deliberate variations. Discussion: The method proved capable of consistently quantifying CoQ10 with superior specificity and sensitivity. Application to commercial soft gel formulations confirmed assay values at 99.5% of the label claim, meeting pharmacopeial standards. Conclusion: This QbD-based RP-HPLC method offers a validated, reproducible, and regulation-compliant strategy for the quality control and stability assessment of CoQ10 dosage forms, with potential extension to similar pharmaceutical compounds.

Formulation development and characterization of flucinolone acetonide nanoemulsion for ocular drug delivery system

Chetan Amrutkar — 2025-10-31

Background: The purpose of this study is to enhance and demonstrate the effectiveness of the corticosteroid drug fluocinolone acetonide in the form of an ophthalmic nanoemulsion. This formulation is designed to improve targeted delivery and ocular penetration, making it suitable for the treatment of conditions such as age-related macular degeneration, diabetic macular edema, and posterior uveitis. Methodology: To formulate the nanoemulsion, we used polysorbate 20 and a castor oil derivative known as HCO-40. The continuous emulsification method was employed to prepare the formulation. Initial batches were tested for key properties, including pH, osmolality, drug content, globule size, and zeta potential. A factorial design approach was applied, in which polysorbate 20 and the castor oil derivative (Cremophor RH 40) were considered independent variables. The nanoemulsion was further evaluated for ocular irritancy using cell line analysis, in vitro scleral permeability, and the Hen’s Egg Chorioallantoic Membrane (HET-CAM) test. Results and Discussion: The optimized batch of the nanoemulsion showed a penetration rate exceeding 80% and a small globule size of 19–20 nm. In vitro tests using human retinal pigment epithelial (ARPE-19) cells and the HET-CAM test indicated that the formulated nanoemulsion is non-toxic and non-irritating to the eye, confirming its cytocompatibility. Conclusion: The developed optimized nanoemulsion formulation of flucinolone acetonide provides improved targeting, non-invasive administration & enhanced patient compliance when used as a topical eye drop for treating ocular diseases such as age-related macular degeneration and posterior uveitis.

Phytochemical profiling and evaluation of in-vitro antidiabetic effects of Pyracantha crenulata (D. Don) M. Roem. fruit extracts

Himani Dumka — 2025-10-31

Background: Pyracantha crenulata (D. Don) M. Roem. is a species of flowering plant, commonly known as Nepalese or Himalayan firethorn, and belongs to the Rosaceae family. Various species of the genus Pyracantha have been reported to reveal antidiabetic activity. The literature suggests that the fruits are conventionally used to reduce blood sugar levels, warranting further research. Therefore, this research provides valuable insights into phytochemical profiling and antidiabetic potential of different extracts of Pyracantha crenulata (D. Don) M. Roem fruits with in vitro models via alpha (α)-amylase and alpha (α)-glucosidase enzyme inhibition assay. Methodology: The successive extraction of Pyracantha crenulata (D. Don) M. Roem fruit was carried out by using different solvents with increasing polarity, including n-hexane, ethyl acetate, ethanol, and distilled water (dH2O) via the Soxhlet extraction technique. The distinct unprocessed extracts were then subjected to a qualitative/quantitative phytochemical investigation of phytonutrients, followed by an assessment of their in vitro antidiabetic potential. Results and Discussion: The results concluded that phytocompounds, including flavonoids, phenols, steroids, and tannins, were tentatively identified in this plant. The extracts inhibit alpha (α)-glucosidase and alpha (α)-amylase enzymes in a dose-dependent way. Among all the extracts, the ethanolic extract exhibited potent anti-diabetic activity, with an IC50 of 44.79 µg/ml at 100 µg/ml in the α-amylase inhibitory assay and 30.09 µg/ml at 100 µg/ml in the α-glucosidase inhibitory assay, which is comparable to that of the standard acarbose. Conclusion: The study demonstrates that ethanolic fruit extract ameliorates hyperglycemia by releasing bioactive substances, providing a rationale for its traditional use as a natural hypoglycemic agent.

Investigation of thiazolidinedione derivatives for anti-diabetic screening: synthesis, in silico analysis, and in vivo evaluation

Gourav Trivedi — 2025-10-31

Background: Diabetics possess inadequate amounts of insulin to control high glucose levels. Current WHO research estimates that 382 million people have diabetes mellitus, and by 2035, 592 million will. Thiazolidinedione, a physiologically active heterocyclic molecule, including thiazolidine-2,4-dione, is being studied for its anti-diabetic action. Thiazolidinediones, a class of hypoglycaemic drugs used to treat noninsulin-dependent diabetes, were first discovered as insulin-sensitive tissue stimulators. Methodology: In-silico applications like Lipinski's rule of five and Molinspiration evaluate physicochemical characteristics, and Molegro Virtual Docker docks molecules. Additionally, compounds are screened in vivo using alloxan as a diabetes inducer and pioglitazone as a comparator medication. Result and Discussion: Docking results determine the interactions of derivatives with 5U5L's active site (H2, H3, H5, H7, H9, and H14). Compound H3 interacts with Cys285, Tyr327, Ser289, His323, and Ala278, whereas compound H14 involves Ser289, Leu353, Phe360, Cys285, and Tyr473 with the PPAR-γ receptor, yielding docking scores of -128.341 and -129.766, respectively, and an RMSD value of 2.55 Å. Docking results showed anti-diabetic effects for H3 and H14. In animal screening, both compounds demonstrated efficacy against alloxan-induced diabetes models, supporting their computational findings. Conclusion: Pioglitazone interacts with hydrogen bonds involving Ser342, Tyr473, Ser289, Glu291, and Leu228 with a docking score of -118.485, while its co-crystal ligand interacts with Tyr327 and Tyr473 with -121.439. This work demonstrates that the thiazolidinedione pharmacophore is crucial for the discovery of anti-diabetic drugs. Both compounds showed significant anti-diabetic effectiveness in computational and in vivo screening. Thus, more research could prove the compound's anti-diabetic properties.

Development and validation of simple HPTLC – UV assay method for determination of quetiapine fumarate concentrations in simulated plasma fluid

Aakanksha Sinha — 2025-10-31

Background: Quetiapine fumarate (QTF) is a high-affinity monoaminergic antagonist selective for serotonin Type 2 (5HT2) and dopamine Type 2 (D2) receptors. In this paper, we formulated and validated a simple, reproducible, and convenient procedure for determining QTF concentration in Simulated Plasma Fluid using HPTLC-UV. Methodology: Simulated plasma samples do not require deproteinization. A simulated plasma fluid sample was prepared using a one-step filtration method with a 0.45 µm nylon syringe filter. HPTLC chromatographic separation of test plasma samples was achieved by TLC silica gel aluminium plates 60 F254, which served as the stationary phase. Results and Discussion: The mobile phase consisted of a mixture of methanol and acetonitrile (3:7 v/v), followed by densitometric detection at 296 nm. Well, separated peaks have been noted with retardation factors (Rf) of 0.62. Calibration plots were found to be highly linear (Correlation coefficient r²> 0.99) in the concentration interval of 20–120 ng/mL. Inter and intraday assay precision and accuracy were below 2%. The proposed method avoided the use of a buffer and employed low volumes of simulated plasma samples with plain mobile phase composition. Conclusion: The developed HPTLC–UV assay method was found to be simple, accurate, and reproducible for determining Quetiapine Fumarate in simulated plasma fluid. Validation results confirmed the method's specificity, linearity, precision, and robustness as per ICH guidelines. This method can be effectively applied in routine bioanalytical studies and drug monitoring.

Pharmacognostic, in vitro antioxidant and hepatoprotective activity of leaves of garden croton, Codiaeum variegatum (Euphorbiaceae)

Swapnil Pandey — 2025-10-31

Background: Commonly referred to as garden croton, Codiaeum variegatum is a tropical decorative plant that is valued for both its therapeutic properties and its colourful foliage. The present study investigates the antioxidant and hepatoprotective properties of garden croton. Methodology: The phytochemical screening was conducted to determine the amount of polyphenols present in the sample. The Total Phenolic and flavonoid content was performed by the Folin and Aluminium chloride method, respectively. Furthermore, the samples were evaluated using various antioxidant methods. Hepatoprotective activities of the crude extract of the plant were carried out based on paracetamol-induced liver damage in mice. Serum biomarkers (AST, ALT, ALP, and hepatotoxicity index) were assessed to determine the effect. Histopathological examination was also performed on all groups of mice to further confirm the findings. Result and Discussion: The different methods revealed that the antioxidant potential increased with higher concentrations of polyphenols in the sample. The IC₅₀ values ranged from 99.28 to 115.22 µg/mL with three different methods. Pre-treatment of the mice with the crude extract of Croton significantly reduced ALP (p < 0.05), ALT (p < 0.05), and AST (p < 0.05) levels at all administered doses compared to the toxic group. Conclusion: Croton leaves may serve as a natural source of novel compounds with hepatoprotective properties. These results suggest that Ornamental plants also contain a higher concentration of bioactive compounds capable of neutralizing free radicals and show hepatoprotective activity at very low doses. However, further research is recommended to isolate and characterize the specific phytoconstituents responsible for the activity and to elucidate their mechanisms of action in greater detail.