Journal of Applied Pharmaceutical Research

Applications of bioactive compounds of traditional Chinese medicine in breast cancer management

Saumya Srivastava — 2025-08-31

Background: Over the past few decades, the prevalence of breast cancer has been rapidly increasing, making it one of the most prevalent malignancies diagnosed in women globally. Traditional Chinese Medicine (TCM) has gained attention as a potential approach for managing breast cancer by boosting immune response, inhibiting cancer-related gene activity, and alleviating the adverse effects of radiotherapy and chemotherapy. TCM offers a valuable framework for therapeutic systems and scientific exploration that is widely practiced in many regions worldwide, primarily in China, Korea, and Japan. The herbal components of TCM exhibit complex biological activities that influence multiple aspects of cancer progression, including cell proliferation, programmed cell death (apoptosis), immune modulation, and tumor-host interactions. Methodology: A systematic literature review was conducted using peer-reviewed articles published between 2017 and 2024. Relevant data were collected from publicly available scientific databases. Non-English, Conference papers, and duplicate studies were excluded to ensure the inclusion of high-quality and relevant research findings. Result and Discussion: Analysis revealed that specific bioactive compounds in TCM exhibit significant anti-cancer effects. For example, ginsenoside Rg3 inhibited tumor growth by 45% in vivo, while curcumin reduced MDA-MB-231 breast cancer cell viability by 60% at 20 μM. Conclusion: The promise of TCM, especially its bioactive components and medicinal herbs in the treatment of breast cancer, is the main highlight of this paper. Additionally, it highlights the key scientific databases that provide critical insights into TCM research while exploring the therapeutic mechanisms of Chinese herbs and their bioactive components in mitigating breast cancer progression.

Scientific perspectives on Guillain-Barre Syndrome (GBS): A comprehensive review for sentience after early 2025 GBS outbreak in an Indian state

Sarika J Patil — 2025-08-31

Background: Guillain-Barré Syndrome (GBS) is an acute, self-limiting, and rare neurological disorder wherein the body's immune system mistakenly attacks the peripheral nervous system (PNS). A report, published in February 2025 by the Indian newspaper ‘The Times of India’, highlighted a significant outbreak of GBS in the Indian state of Maharashtra, owing to the Campylobacter jejuni (C. jejuni) infection. The surge in cases has been considered as one of the most significant recorded GBS outbreaks globally, which underscores the need to raise GBS awareness. Method: This article provides an in-depth scientific perspective on GBS, drawing on literature from scientific databases such as PubMed and ScienceDirect. It aims to enhance awareness among science-related students, researchers, medical and paramedical professionals, and the general public. Result and discussion: GBS is an acute polyneuropathy characterized by limb weakness with hyporeflexia or areflexia. In severe forms, respiratory and bulbar paralysis can occur, requiring mechanical ventilatory support. It is the commonest cause of acute neuromuscular paralysis. The basic underlying mechanism of the disease is a localized attack against the myelin sheath of the peripheral nerves and nerve roots, with secondary axonal damage. It is believed that the bacterial antigens have a close molecular mimicry with neural antigens. As a result, the response generated against these antigens cross-reacts with the neural cells. Plasma exchange, immunoglobulin infusion, and plasmapheresis are the mainstays of treatment for GBS. Conclusion: A thorough understanding of GBS is essential, including its pathophysiology, underlying causes, risk factors, symptoms, diagnostic methods, treatment strategies, and the latest advancements.

Formulation and evaluation of a bifonazole-loaded chitosan-honey invasomal hydrogel for enhanced topical antifungal activity

Shivaji Patil — 2025-08-31

Background: To develop a novel bifonazole-loaded chitosan-honey invasomal hydrogel to improve the drug's topical antifungal efficacy. In this formulation, invasomal vesicles, composed of phospholipids, ethanol, and terpenes, were utilized to enhance the penetration of bifonazole through the skin. Methodology: These invasomal carriers were incorporated into a chitosan-based hydrogel matrix, which provided structural stability and bioadhesive properties, allowing for better retention on the skin. Additionally, natural honey, known for its antibacterial and wound-healing properties, was included to enhance the therapeutic benefits of the hydrogel. Results & Discussion: Invasomes were prepared using soya phosphatidylcholine, ethanol (30% v/v), and d-limonene (0.5%) and then incorporated into a chitosan-honey gel matrix. Among the six formulations (IF1–IF6), IF5 showed optimal results, with 93.32% drug release over 12 hours, a viscosity of 6545 ± 26 cps, a pH of 6.85, and antifungal inhibition zones of 17 mm (Candida albicans) and 11 mm (A. flavus). The formulation was characterized in terms of its physical properties, including viscosity, gel strength, and spreadability, and evaluated for its drug entrapment efficiency, in vitro drug release profile, and ex vivo skin permeation. This study demonstrates a synergistic system enhancing skin permeation, drug retention, and antifungal efficacy. Conclusion: This formulation represents a promising alternative for the effective and patient-friendly treatment of superficial fungal infections, offering improved drug delivery, enhanced therapeutic efficacy, and a reduced dosing frequency.

Transdermal delivery of risedronate using chemical enhancers for improved skin penetration

So Hee Nam — 2025-08-31

Background: Risedronate sodium (RIS) is effective for bone diseases but has low bioavailability and severe side effects. This study investigates the use of hydrophilic enhancers to improve the efficiency of RIS's transdermal delivery. Methods: This study involved preparing topical samples of RIS with various enhancers, including ethanol (EtOH), dimethyl sulfoxide (DMSO), Dimethylene glycol monomethyl ether (DGME), and propylene glycol (PG). In vitro permeation tests were conducted using hairless mouse skin in Franz diffusion cells, and skin irritation tests were performed on mice. Results: The cumulative amount of RIS after 24 hours significantly increased with penetration enhancers: 6.02 μg/cm² (RIS alone), 90.22 μg/cm² (20% DGME), 67.31 μg/cm² (20% PG), 266.31 μg/cm² (20% DMSO), and 784.52 μg/cm² (20% EtOH). EtOH showed a dose-dependent increase, with 1,302.76 μg/cm² at 50% concentration. Further experiments using DMSO and EtOH at concentrations of 5% and 10% identified the optimal permeation enhancement as follows: 201.36 ± 31.6 μg/cm² (5% DMSO), 183.03 ± 31.6 μg/cm² (10% DMSO), 261.71 ± 164.93 μg/cm² (5% EtOH), 569.21 ± 197.67 μg/cm²(10% EtOH). Discussion: EtOH and DMSO significantly enhanced RIS penetration by modifying the skin's structure. The study suggests that adjusting the concentration of these enhancers can control the penetration profile, offering a promising alternative to oral delivery. Conclusions: This study demonstrated that chemical enhancers significantly improved the skin penetration of RIS. The transdermal delivery of RIS can help reduce the side effects of oral delivery of the drug and thus improve patients’ compliance.

Preliminary phytochemical screening, FT-IR, and HPTLC analysis, and antioxidant, antimicrobial activities of methanolic extracts of Dalbergia sisso leaves

Varun Chaddha — 2025-08-31

Background: Dalbergia sissoo is a well-known plant known as Shisham. It has medicinal importance, including analgesic, antipyretic, and antiemetic properties. Therefore, the primary objective of this research is to investigate the bioactive constituents in the methanolic leaf extract of Dalbergia sisso by characterizing it using FT-IR and HPTLC techniques, and to determine its antioxidant and antimicrobial activities. Methodology: A Soxhlet apparatus was used for the extraction process. 150 g of Dalbergia sisso powdered leaves was extracted using a Soxhlet apparatus for 30 hours, utilizing methanol as a solvent. The solvent was vaporized and concentrated to produce a dry residue once the extraction was finished. The yield percentages for the methanolic extract were 4.8% respectively. Result and Discussion: FT-IR spectroscopy showed different peak values for functional compounds in the methanolic extract. The FTIR spectrum of the methanolic leaf extract shows the interpretation of the chemical bonds in the methanolic leaf extract. HPTLC studies revealed that the active compound lupeol is present in the methanolic extract. Conclusion: It has been concluded that the methanolic extract of Dalbergia sisso leaves contains lupeol and quercetin bioactive compounds. The methanolic extract of Dalbergia sisso leaves was found to have antioxidant and antimicrobial effects. The HPTLC technique found lupeol, which may possess antioxidant and antimicrobial activities. The FT-IR spectrum revealed the presence of hydroxyl, hydrocarbon, aldehyde, allene, and secondary alcohol groups in the methanolic extract, consistent with the presence of quercetin. The methanolic leaf extracts show the presence of saponin, alkaloids, flavonoids, anthraquinone glycosides, and tannins.

Pharmacognostical, phytochemical, and in vitro bioassay studies of Osbeckia stellata Buch-ham. leaves

Chayanika Bordoloi — 2025-08-31

Background: Osbeckia stellata (Os) is a medicinally significant herb that is consumed for the treatment of various diseases, including skin diseases, diabetes, diarrhea, cancer, asthma, arthritis, dysentery, leukoderma, hypertension, jaundice, malaria, rheumatism, spondylitis, and tuberculosis, as well as inflammation and wound healing. Methodology: This study standardizes the plant of Os by accepted practices. Os leaves have been examined physicochemically, phytochemically, microscopically, and morphologically. Extracts were reviewed for both qualitative and quantitative phytochemical examination, and in vitro bioassays were also evaluated. Results: Diagnostic traits, such as xylem arteries, trichomes with cover, and anomocytic stomata, were identified in the histological study. Nutritional profiling revealed fiber content (48.1 ± 0.99 mg/100 g). Heavy metal analysis revealed that Pb, Hg, Sn, Sb, Cd, Cu, and As were within the permissible limits. Pesticide residues were verified with ICP-MS analysis. The in vitro antioxidant studies of different extracts show IC₅₀ values 1003.35±0.23, 152.11±0.1, 192.12±0.14, 111.79±0.06, and 982.49±0.31 (μg/ml) as compared to standard 130.54±0.03 and 330.86±0.09 (μg/ml). Antimicrobial assay studies show the Zone of Inhibition by different extracts is 26.00 ± 1.20, 17.00 ± 0.60, 18.66 ± 0.58, 22.33 ± 1.52, 6.33 ± 0.58 (mm) as compared to the standard 38.00 ± 1.00, 35.00 ± 1.35, 22.00 ± 1.00, 41.00 ± 1.00, 30.66 ± 1.54(mm). Discussion: The methanol extract of Os has total phenols and total tannins of 120.04±5.97 and 123.0±1.52 (mg/g TAE), respectively, which is high in quantity and is reported to possess high antimicrobial and antioxidant properties. Conclusion: This study concludes that the quality control parameters for Os are essential for promoting its use in pharmaceutical applications.

Mechanical and dissolution properties of Eudragit L100 and S100 films in buffer solutions

Vaibhav Jindas Ambudkar — 2025-08-31

Background: Methacrylic acid (MAA) and methyl methacrylate (MMA) affect the mechanical and dissolution properties of enteric polymers, such as Eudragit L100 and S100. Their composition determines polymer flexibility, strength, and solubility, which are critical for pharmaceutical enteric coatings. This study examines the impact of the MAA: MMA ratio on the mechanical and dissolution properties of Eudragit L100 (1:1) and Eudragit S100 (1:2) films. Methodology: Mechanical testing assessed stiffness, tensile strength, and flexibility. Dissolution studies evaluated solubility at different pH levels, measuring peak dissolution rates. Results and Discussion: Eudragit L100, with more MAA, was stiffer and more brittle, while Eudragit S100 had higher tensile strength but reduced flexibility. Acidic conditions weakened both, due to water interactions with MAA. Eudragit L100 dissolved rapidly at pH 7.2 (90% mass loss in 60 min, peak 30.4 mg/g·min at 10 min), whereas Eudragit S100 showed minimal dissolution at lower pH, but dissolved significantly at pH 8.0 (64.5% at 180 min, peak 6.7 mg/g·min at 30 min). Larger dissolution volumes, maintained concentration gradients, enhancing dissolution, while high-capacity buffers stabilized pH and improved solubility. Conclusion: MAA: MMA composition critically affects the mechanical and dissolution properties of Eudragit L100 and S100, with concentration gradients playing a key role in dissolution, informing their application in enteric coatings.

Neuroprotective potential of methanolic leaf extracts of Celosia cristata and Callistemon citrinus on scopolamine-induced amnesia in swiss albino mice

Vishwambhar Mishra — 2025-08-31

Background: The primary reason for memory loss is Alzheimer’s disease, a progressive neurodegenerative condition in specific brain parts. This study aims to illustrate the relative enhancement of memory, along with the neuroprotective and antioxidant properties of methanolic leaf extracts from Celosia cristata and Callistemon citrinus in scopolamine-induced amnesia in mice. Methodology: Methanolic extracts of the leaves of Celosia cristata and Callistemon citrinus were evaluated for their effects on scopolamine-induced impaired learning and memory in Swiss albino mice using behavioral animal models, including the Morris water maze (MWM), elevated plus maze (EPM), and object recognition task (ORT). Antioxidants such as Superoxide dismutase (SOD), Glutathione peroxidase (GPx), Thiobarbituric acid reactive substance (TBARS), and acetylcholinesterase (AChE) were also assessed at different doses, i.e., 200 and 400 mg/Kg of methanolic extracts of Celosia cristata and Callistemon citrinus, as well as their combinations. Results and Discussion: The various doses of Celosia cristata and Callistemon citrinus methanolic leaf extracts significantly modified scopolamine effects in experimental animals. Extracts significantly decreased escape latency (ELT) in the MWM test. Inflexion ratio (IR) in the EPM test was significantly raised by extracts, as well as the discrimination index (DI) in ORT. The SOD and GPx levels were significantly enhanced whereas TBARS significantly reduced by extracts. The significant reduced level of AChE was reported in extract treated mice. The extracts from both plants exhibited significant results at different doses (200 mg/kg and 400 mg/kg) and combination of both plant extracts (MCel+MCal 400) at 400mg/kg dose showed most significant result. Conclusion: The results revealed that methanolic leaf extracts of Celosia cristata and Callistemon citrinus hold potent antiamnesic effects.

Antimicrobial potential, GC-MS analysis, and molecular docking studies of Pogostemon benghalensis leaf extract

Bhaswati Kashyap — 2025-08-31

Background: Pogostemon benghalensis has several medicinal uses in Northeast India, including wound healing activity. Currently, no molecular modeling research has examined the antimicrobial potential of its phytoconstituents. This molecular docking research identifies bioactive chemicals and evaluates their antibacterial properties. Methodology: Phytochemical screening and in vitro antibacterial tests were performed on a crude ethyl acetate extract of Pogostemon benghalensis leaves. After GC-MS analysis revealed the phytoconstituents, in-silico molecular docking was performed against the dihydrofolate reductase (DHFR) enzymes of Escherichia coli and Staphylococcus aureus. Results and discussion: The crude ethyl acetate extract of Pogostemon benghalensis leaves included alkaloids, carbohydrates, flavonoids, glycosides, tannins, and phenolic compounds. The extract also demonstrated potent in vitro antibacterial activity against E. coli and S. aureus. GC-MS data demonstrated that Phytol was the most abundant compound (53.72%) followed by Oxirane, dodecyl (13.51%.). Molecular docking studies demonstrated identified compounds have high binding affinity (BA) to the bacterial DHFR enzyme. Notable compounds are Androst-5-ene-3,19-diol, 3-acetate (3 β) with -7.4 kcal/mol BA against E. coli DHFR and -10.1kcal/mol against S. aureus DHFR; Retinol acetate with -8.7 kcal/mol BA against E. coli DHFR and Phytol with -6.5 kcal/mol BA against E. coli DHFR and -6.7 kcal/mol BA for S. aureus DHFR respectively. Conclusion: The results show that Pogostemon benghalensis contains valuable bioactive compounds with high antibacterial activity which further validates the use of this plant as a wound healing medication. However, further in vivo experimental validation of these results and their toxicological implications are required.

Formulation development and evaluation of oil-based PLGA nanocarriers of fluticasone propionate

Aniruddha Shejwal — 2025-08-31

Background: Fluticasone Propionate (FP), a potent corticosteroid, suffers from poor aqueous solubility and limited skin permeability, which reduces its clinical efficacy in topical applications. This work aims to overcome these limitations; oil-based poly(lactic-co-glycolic acid) (PLGA) nanocarriers were developed to enhance the solubility, stability, and sustained release of FP. Methodology: A 3² factorial design was employed to formulate nine batches of PLGA nanocarriers loaded with FP using varying concentrations of PLGA and Capmul MCM. The formulations were evaluated for particle size, zeta potential, drug content, and in vitro drug release. The optimized batch was further characterized using Scanning Electron Microscopy (SEM), Differential Scanning Calorimetry (DSC), and X-Ray Diffraction (XRD). Stability studies were conducted over 30 days under accelerated conditions. Results and Discussion: Among all batches, formulation F1 exhibited optimal characteristics, with a particle size of 197.5 nm, a zeta potential of -27.4 mV, and a drug content of 99.85%. The in vitro drug release profile showed a sustained release of 97% over 12 hours. SEM confirmed a spherical morphology with uniform distribution, while DSC and XRD analyses indicated the amorphous dispersion of the drug within the PLGA matrix. The formulation remained physically and chemically stable during the 30-day accelerated stability testing. Conclusion: The study demonstrates that oil-based PLGA nanocarriers effectively enhance the solubility and controlled delivery of Fluticasone Propionate. Although in vivo validation is pending, the system offers promising potential for improving topical corticosteroid therapy in clinical settings. The novelty of this formulation lies in the strategic combination of Isopropyl Myristate and PLGA to create an oil-based nanocarrier platform, which has not been previously reported for Fluticasone Propionate. This approach enables superior drug encapsulation, enhanced skin permeability, and controlled drug delivery.

Chromatographic profiling of leniolisib impurities using HPLC and LC-MS/MS: degradation behaviour, structural characterization, and in-silico toxicity evaluation

Rahul Gunupati — 2025-08-31

Background: This study presents a comprehensive analytical investigation of leniolisib, focusing on impurity profiling, degradation kinetics, structural characterization, and in silico toxicity prediction of degradation products (DPs). Methodology: A systematic approach was employed to optimize the analytical method for leniolisib and its impurities, along with LC–MS/MS-based identification and in-silico toxicity prediction of DPs. Result and Discussion: Method optimized as Waters Symmetry C18 column and an isocratic mobile phase (methanol: sodium acetate buffer, 55:45 v/v) at 0.90 mL/min with UV detection at 229 nm. Leniolisib was most susceptible to acid and oxidative stress, resulting in 31.24% and 39.58% degradation, respectively. Pseudo-first-order kinetics was observed with rate constants of 0.0329 h⁻¹ (acidic) and 0.0414 h⁻¹ (oxidative), with half life of 21.08 h and 16.73 h. LC–MS/MS elucidates the identities of major DPs that enable the proposed degradation pathways. The MS/MS characterization confirms DP 1 with a formula of C₁₃H₁₅N₅O with a mass of 257 g/mol, whereas DP 2, 3, and 4 were identified to have formulas of C₂₀H₂₆N₆O₂, C₁₃H₁₂F₃N₅O, and C₁₇H₁₉F₃N₆O with masses of 382, 311, and 380 g/mol, respectively. The In-silico toxicity predictions show DP 1 (LD₅₀ = 500 mg/kg) and DP 2 (729 mg/kg) as moderate toxicity (class 4), DP 4 shows the least toxicity (class 5, LD₅₀ = 1750 mg/kg), whereas DP3 shows the highest toxicity (class 3, LD₅₀ = 250 mg/kg). Conclusion: The developed method and accompanying data provide a critical foundation for routine quality control, stability testing, and regulatory submissions for leniolisib-based formulations.

Phytochemical profiling and antioxidant evaluation of root ethanol extract of Maesa indica (Roxb.) sweet

Pooja K P — 2025-08-31

Background: Healing herbs have long been used in traditional medicine due to their therapeutic properties and rich content of bioactive molecules. Despite its traditional applications, research on the root part of Maesa indica is scarce. This study focuses on exploring the phytochemical composition and antioxidant potential of the ethanol extract of M. indica roots. Methodology: Secondary metabolites were identified using Liquid Chromatography–Quadrupole Time-of-Flight Mass Spectrometry (LC-Q-TOF-MS). Antioxidant activities were evaluated using the 2,2-diphenyl-1-picrylhydrazyl (DPPH) radical scavenging assay and the metal chelating activity assay. Quantification of total phenolic content (TPC) and flavonoids was also conducted. Results and Discussion: Preliminary phytochemical analysis revealed the presence of flavonoids, phenols, steroids, and saponins. LC-Q-TOF-MS profiling identified seven primary secondary metabolites. The root extract exhibited high phenolic content (380.91 ± 23.52 µg/mg) and moderate flavonoid concentration (114.21 ± 6.25 µg/mg). Antioxidant activity of root extract was demonstrated by DPPH radical scavenging showed strong activity (IC₅₀: 88.78 µg/mL) and moderate ferrous ion chelating activity (IC₅₀: 172.31 µg/mL), suggesting effective free radical neutralization. Conclusion: The findings highlight the root extract of M. indica as a promising source of natural antioxidants. Compared to previous studies on aerial parts of the plant, the root extract offers comparable or enhanced antioxidant capacity, suggesting its value in future pharmaceutical and nutraceutical formulations

Investigation of potential efficacy of nanospanlastic vesicular drug delivery system for targeting the brain: formulation, characterization, and in-vivo studies

Ashwini Patel — 2025-08-31

Background: Edaravone, a potent antioxidant, has limited brain bioavailability due to poor solubility and restricted permeability across the blood-brain barrier (BBB). Intranasal delivery offers a promising alternative for brain targeting by bypassing the BBB. Objective: To develop and evaluate a nanospanlastic-based in-situ nasal gel formulation of edaravone for enhanced brain delivery. Methodology: A Quality by Design (QbD) approach was employed to identify and optimize critical formulation variables using Plackett-Burman and Central Composite Design. The optimized nanospanlastics were incorporated into a gellan gum-based ion-activated in-situ nasal gel and characterized through in vitro, ex vivo, and in vivo studies. Results and Discussion: The optimized formulation exhibited a particle size of 213.4 nm, a drug entrapment efficiency of 67.59%, and rapid gelation upon contact with nasal fluid. In vitro diffusion showed over 80% drug release within 30 minutes, while ex vivo studies confirmed improved permeation (flux: 7.8067 µg/cm²/hr). Histopathology revealed no nasal mucosal irritation. Pharmacokinetic studies in rats demonstrated significantly enhanced brain and plasma exposure compared to the marketed edaravone injection, with higher Cmax (78.73 ng/mL), Tmax (121.2 min), and AUC. Conclusion: The developed nanospanlastic-based nasal gel offers a non-invasive, effective strategy for brain delivery of edaravone, with potential to improve therapeutic outcomes in neurological disorders.

A QbD-based stability-indicating RP-HPLC method for larotrectinib: degradation kinetics and integrated white, green, and blue analytical assessment

Syamala P. N. S — 2025-08-31

Background: Larotrectinib, a selective TRK inhibitor, received FDA approval on April 10, 2025, for treating solid tumors with NTRK gene fusions. Despite its therapeutic significance, no RP-HPLC method using a Quality-by-Design (QbD) framework has been reported. This study aimed to develop and validate a QbD-based RP-HPLC method for larotrectinib estimation. Methodology: Critical Analytical Parameters (CAPs) were identified using a Plackett–Burman Design and optimized via a Central Composite Design (CCD). Separation was achieved on a Sunfire C18 column (250 × 4.6 mm, 5 µm) with a mobile phase of 0.1% OPA and acetonitrile (70:30, v/v), flow rate 1.0 mL/min, injection volume 10 µL, and detection at 262 nm. Optimized conditions from the Method Operable Design Region (MODR) gave a desirability value of 1. Results and Discussion: The method achieved sharp separation with a retention time of 2.2 min in a 5-minute runtime. Validation per ICH Q2(R1) confirmed linearity (12.5–75 µg/mL, R² = 0.9998), intra- and inter-day precision (%RSD < 2%), mean recovery of 99.29%, and sensitivity with DL 0.30 µg/mL and QL 0.92 µg/mL. Forced degradation studies revealed zero-order kinetics under 0.1 N HCl, 0.5 N NaOH, and thermal stress, and first-order kinetics under 0.5 N HCl, 0.1N NaOH, 3% and 5% H₂O₂, and water. Greenness, blueness, whiteness, and sustainability were assessed using AMGS, AGREE, ComplexMoGAPI, BAGI, RGB, and EVG tools, yielding favourable outcomes. Conclusion: The developed QbD-based RP-HPLC method is robust, validated, and stability-indicating, suitable for quality control, regulatory submissions, and bioanalysis of larotrectinib.

In silico assessment of flavonoids from Matricaria chamomilla for anti-psoriatic potential via molecular docking and ADME/T profiling

V. V. Rajesham — 2025-08-31

Background: Computational tools are advancing in the drug discovery process to assess the safety profiles of new compounds with reduced investment. Herbal remedies exhibit a diverse range of active compounds that can alleviate various disease conditions with fewer side effects. Method: This study investigates the molecular docking of phytochemicals from Matricaria Chamomilla against inflammation-induced skin disorders, such as psoriasis. Using AutoDock Vina and MGL Tools, key compounds were evaluated for binding affinity with target proteins. ADMET analysis, as assessed by pkCSM and SWISSADME, to predict the Lipinski’s Rule of Five. Redocking was implemented to confirm the binding affinity of the docked position. Results: This molecular docking of phenolic compounds and flavonoids, including quercetin, apigenin, rutin, luteolin, and various glycosylated derivatives—from Matricaria Chamomilla against cellular proteins implicated in psoriasis (PDE-4, p38MAPK, IL-23, BTK, JAK-3, TNF-α, IL-17A, and IL-6). Using Autodock Vina and MGL Tools, rutin and quercetin demonstrated favourable binding affinities. At the same time, luteolin-7-glycoside exhibited the highest docking scores (e.g., -10.8 kcal/mol for PDE-4, -9.7 kcal/mol for JAK-3, and -9.1 kcal/mol for TNF-α) compared to the standard. Results highlight the potential of chamomile phytochemicals as safe, orally effective agents for managing inflammatory skin conditions. Redocking confirms the RMSD values are within the limits of < 2 A⁰. Conclusion: The data suggest that chamomile flavonoids could be safe and beneficial for treating inflammatory diseases and psoriasis. Although enzymatic and cell-based assays, along with further preclinical evaluations, are essential for advancing research in disease modification, formulation strategies play a role in improving drug characteristics

RP-HPLC method for quantitative estimation of naftifine hydrochloride in formulated products: development and validation

Kajal Sunil Shinde — 2025-08-31

Background: Naftifine hydrochloride is an allylamine antifungal agent commonly used to treat dermatophyte infections. It inhibits squalene epoxidase, a key enzyme in ergosterol biosynthesis, thereby disrupting the integrity of the fungal cell membrane. It exhibits broad-spectrum activity against dermatophytes, yeasts, and molds, and is typically formulated as a 1% topical cream or gel. Methodology: A rapid and robust reverse-phase high-performance liquid chromatography (RP-HPLC) method was developed and validated for the estimation of naftifine hydrochloride in a topical cream formulation (2% Naftifast, Zydus), in accordance with ICH and FDA guidelines. Chromatographic separation was achieved on an Inertsil ODS column using an isocratic mobile phase consisting of 35% acetonitrile, 40% methanol, 25% water, and 0.8% triethylamine (pH adjusted to 5.5 with acetic acid) at a flow rate of 1.4 mL/min. Detection was performed at 265 nm. Results and Discussion: Naftifine hydrochloride showed a retention time of approximately 4.0 minutes with a total run time of 6.0 minutes. The method displayed excellent linearity over a concentration range of 20–120 µg/mL (R² > 0.999). Recovery studies indicated a mean recovery of 100.4%. Precision was confirmed by relative standard deviation (RSD) values of less than 2%, demonstrating the method’s reproducibility. Conclusion: The proposed RP-HPLC method is simple, precise, and time-efficient. It is suitable for routine quality control of naftifine hydrochloride in pharmaceutical dosage forms due to its short analysis time and strong validation performance.

Neuroprotective insights into Agave cantala: dual modulation of neuroinflammation and oxidative stress by phytochemicals through integrated in silico and in vitro approaches

P. Thamarai Selvi — 2025-08-31

Background: Neurodegenerative disorders such as Alzheimer’s and Parkinson’s are strongly associated with chronic neuroinflammation and oxidative stress. Phytochemicals from medicinal plants offer promising multitarget therapeutic potential. Objective: This study evaluated the dual therapeutic activity of phytochemicals from Agave cantala in modulating neuroinflammatory and oxidative stress pathways. Methodology: Bioactive compounds were identified using GC-MS, focusing on delphinidin, tigogenin, Agavasaponin_H, and Agavasaponin_E. Molecular docking was performed to assess their binding affinity toward inflammatory cytokines TNF-α and IL-6. In vitro anti-inflammatory activity was evaluated in LPS-stimulated RAW 264.7 macrophages by measuring TNF-α and IL-6 levels. Antioxidant activity was assessed through DPPH, ABTS, and FRAP assays. Results and Discussion: Docking studies revealed strong interactions of delphinidin and tigogenin with TNF-α and IL-6, suggesting effective inhibition. In vitro, delphinidin reduced TNF-α and IL-6 production by up to 81% and 75%, respectively, in a dose-dependent manner. Tigogenin and the saponins also showed notable cytokine suppression. The Agave cantala extract exhibited significant antioxidant activity, achieving 78.3% radical scavenging in the DPPH assay at 100 μg/mL. These results indicate that the identified phytochemicals modulate key inflammatory and oxidative pathways, supporting their multitarget action. Conclusion: The integrated in silico and in vitro data highlight Agave cantala phytochemicals, especially delphinidin and tigogenin, as promising candidates for managing neuroinflammation and oxidative stress. Further in vivo validation and pharmacokinetic profiling are recommended to support their clinical potential.

Development and in vitro evaluation of liquid crystal-based polyherbal hair gels: physicochemical characterization, hair performance, and antioxidant assessment

Sheba R David — 2025-08-31

Background: A liquid crystal (LC) based polyherbal hair gel was developed to enhance physicochemical stability and functional performance in topical hair care. The objective was to integrate herbal oils (flaxseed, coconut, and almond) and aqueous extracts (green tea, keratin hydrolysate, and pea peptide), known for their moisturizing, antioxidant, follicle-protective, and anti-frizz effects, into a stable gel matrix for scalp care and conditioning. Methodology: Ten formulations (F1–F10) incorporating flaxseed, coconut, and almond oils with green tea, marula extract (Sclerocarya birrea), keratin hydrolysate, and pea extract were prepared via coacervation, vortex mixing, and high-pressure homogenization. The gels were evaluated for their organoleptic properties, pH, spreadability, particle size (as determined by dynamic light scattering, DLS), polydispersity index (PDI), and zeta potential. Polarized Light Microscopy and FTIR characterized structural features. Functional performance was evaluated by in vitro studies on hair diameter and weight changes, as well as anti-frizz, anti-static, and antioxidant (DPPH) activities. Results and Discussion: Formulation F6 showed optimal nanometric characteristics (186.47 ± 1.90 nm, PDI 0.351 ± 0.01, zeta potential −35.9 mV), indicating stable colloidal dispersion. FTIR and microscopy confirmed molecular compatibility and mesophase birefringence. In vitro assessments revealed marked improvement in hair thickness for F6 and F9, with superior anti-frizz and anti-static performance for F4 and F9. Antioxidant activity was moderate compared to Trolox. F4 and F6 maintained stability over 28 days at different temperatures. Conclusion: F4 and F6 demonstrated superior in vitro performance and stability, suggesting promise as cosmeceutical hair care candidates. In vivo and clinical studies are required to confirm efficacy and long-term safety.

In vitro anticancer potential of Manilkara hexandra (Roxb.) leaf methanolic extracts via SRB and MTT assays against MCF-7 cell line

Sunayana R. Vikhe — 2025-08-31

Background: Cancer causes millions of deaths worldwide, with cases expected to reach 28.4 million by 2040. Natural plant compounds offer safer alternatives for cancer treatment. Aim: This study tested the anticancer activity of Manilkara hexandra leaf extracts against MCF-7 breast cancer cells. Materials and methods: Methanolic extraction, followed by sequential fractionation via column chromatography, yielded bioactive fractions that underwent phytochemical and GC-MS characterization. Quantification of cytotoxicity was performed using sulforhodamine B (SRB) and 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide (MTT) assays across a concentration gradient (10–80 μg/mL). Result and Discussion: Chemical screening found alkaloids, flavonoids, tannins, and other bioactive compounds. The petroleum ether-ethyl acetate (PE-EA) fraction contained quercetin (25.28%) and another major flavonoid (28.62%). This fraction exhibited strong dose-dependent cell killing, reducing cell survival to 31.8% (SRB) and 33.0% (MTT) at 80 μg/mL (p < 0.001). The IC₅₀ was 55 μg/mL in both assays. Conclusion: The anticancer activity correlates with high flavonoid content, suggesting these compounds cause cell death through apoptosis or cell cycle arrest. M. hexandra PE-EA fraction shows promise as a natural anticancer agent for breast cancer treatment

Design, optimization, and antimicrobial assessment of Callicarpa longifolia-derived nanoparticles using quality by design (QbD) approach

Md. Shakeel Alam — 2025-08-31

Background: The purpose of this study is to focus on the design, optimization, and antimicrobial evaluation of ethanolic leaf extracts of Callicarpa longifolia-derived nanoparticles using the Quality by Design (QbD) technique. Methodology: Critical formulation parameters were optimized using a Box-Behnken Design. The optimized nanoparticles are characterized using Dynamic Light Scattering (DLS), Zeta Potential analysis, and Scanning Electron Microscopy (SEM), confirming their nanoscale size. Stability studies were conducted under various ICH recommendations. The antimicrobial activity of the isolated fraction extract and isolated fraction extract nanoparticles was assessed against Gram-positive (Staphylococcus aureus) and Gram-negative (Escherichia coli) bacteria using the agar well diffusion method. Results and Discussion: By BBD, the optimized herbal nanoparticles have a particle size of 281.00 nm and an entrapment efficiency 88%. After characterization, the results of the optimized nanoparticles' particle size (349.3 nm), zeta potentials (-23.7 mV), % EE (86.25%), and spherical shape are confirmed by SEM. The % cumulative drug release of optimized nanoparticles is 86.12±0.79. Kinetic release model regression values of the optimized nanoparticles' R² values in different model kinetic releases are zero order (0.929), first order (0.971), Higuchi kinetic release (0.994), Korsmeyer kinetic release (0.994), and Hixon Crowell (0.978). Results revealed that the nanoparticle formulation exhibited significant antimicrobial efficacy. Conclusion: All things considered, the study shows how the QbD methodology may be successfully applied to create a stable and efficient nanoparticle system made from an isolated extract of C. longifolia, which has encouraging potential as a substitute antibacterial agent.

Innovative nanostructured lipid carrier gel for enhanced topical delivery of roflumilast in psoriasis management

Abhishek Singh — 2025-08-31

Background: Psoriasis is a chronic immune-mediated skin disorder marked by keratinocyte hyperproliferation, inflammation, and oxidative stress, causing erythematous, scaly plaques that impair quality of life. Current therapies have side effects and poor solubility, highlighting the need for improved topical delivery systems. Methodology: An NLC-based gel encapsulating the PDE4 inhibitor roflumilast was developed for enhanced topical delivery. NLCs were prepared by high-pressure homogenization with oleic acid, glycerol monostearate, and Tween 80, and incorporated into a Carbopol 934 gel. The physicochemical properties, encapsulation efficiency, in vitro release, and in vivo efficacy of imiquimod in imiquimod-induced psoriatic rats were evaluated. Results: The developed gel was homogeneous, white, and transparent, with a dermally compatible pH (5.36-5.85), optimal viscosity (3.5-14.5 Pa·s), and good spreadability (4.3-7.2 g/cm/s). Formulation F3 showed high encapsulation efficiency (90.38 ± 2.91%) and sustained drug release (~90% over 24 hours). Drug content ranged from 72% to 95%. Ex vivo skin permeation studies demonstrated enhanced roflumilast penetration. In vivo application led to a significant reduction in psoriasis area and severity index (PASI) scores from 6.5 on Day 1 to 1.6 on Day 9. No signs of erythema, edema, or rashes were observed during the 72-hour skin irritation study, confirming excellent dermal compatibility. Histopathology confirmed decreased inflammation, reduced hyperkeratosis, and restored epidermal architecture. Discussion: The NLC-based roflumilast gel showed favorable physicochemical and biopharmaceutical properties, offering improved delivery and sustained release over conventional psoriasis therapies. Conclusion: Roflumilast-NLC gel is a promising topical therapy for psoriasis with controlled release and enhanced skin retention.

Chitosan-based mucoadhesive patches for buccal delivery of olmesartan in hypertension treatment

Ram Nikhate — 2025-08-31

Background: Delivering poorly soluble drugs like Olmesartan (OMS) effectively remains a key challenge due to low oral bioavailability and extensive first-pass metabolism. To address this, buccal patches incorporating chitosan were developed as an alternative route to enhance systemic absorption. Methodology: A series of buccal patch formulations (F1–F17) was prepared using combinations of chitosan, polyvinyl alcohol (PVA), HPMC K4M, and Eudragit RL via solvent casting. These patches were evaluated for uniformity in weight, thickness, pH, mechanical strength, folding endurance, and mucoadhesion. Structural and morphological assessments were carried out using X-ray diffraction and SEM. Ex vivo and in vivo studies explored drug release, permeation, pharmacokinetics, and mucosal safety. An HPLC method was employed for accurate quantification, and stability was assessed under both accelerated and ambient conditions. Results and Discussion: The optimised patch (F2) demonstrated consistent physical properties, high flexibility, and strong mucoadhesion. XRD patterns confirmed the amorphous dispersion of OMS in the polymer matrix, aiding solubility. Drug release was sustained over 12 hours, and permeation studies showed controlled transport across the buccal membrane. In vivo results revealed a substantial improvement in drug bioavailability via buccal delivery (83.2%) compared to oral administration (30.2%). Histological analysis indicated no signs of tissue irritation. Patches maintained integrity and potency throughout six months of storage. Conclusion: The findings support the buccal patch as a viable, non-invasive platform for enhancing OMS delivery, offering improved therapeutic efficiency and patient compliance.

Development of abemaciclib-encapsulated nanosponges for breast cancer: optimization, drug release kinetics, and in vitro efficacy

Nirosha Bolledla — 2025-08-31

Background: Abemaciclib (ABC) is a new, orally administered pharmaceutical agent authorised for the purpose of combating breast cancer. The drug's low bioavailability necessitates dosing two to three times daily, which may reduce patient compliance. To lessen the severity of side effects and prolong the duration of action, sustained-release formulations are required. Developing an ABC sustained-release nanoparticle system was the primary goal of this study. Methodology: Both the sustained-release polymer (EC) and the surfactant (KP-188) were derived from ethyl cellulose, in an emulsion-solvent diffusion synthesis of nanosponges (NS). We examined the impact of varying surfactant concentrations and drug-to-polymer ratios on PS, PDI, ZP, %EE, %DL, particle size, drug loading, zeta potential, and polydispersity index. Results and Discussion: The optimized formulation (F11) achieved an entrapment efficiency of 86.52±0.25% and a cumulative drug release of 77.12% over 24 hours. The drug release followed a sustained pattern over 24 hours. It best fits the Higuchi kinetic model, which indicates that drug diffusion was the primary mechanism of release from the matrix system. The MTT experiment demonstrated that ABC might be a viable cytotoxic nanocarrier for breast cancer cells from humans, specifically MCF-7 and MDA-MB-231. On top of that, following contact with storage settings of 25, 5, and 45 °C for six months, ABC maintained its drug release property with no modification in the percentage release. Conclusion: This study shows that the created NS could effectively transport and release ABC, amplifying its impact in the battle against breast cancer.

Formulation, designing and evaluation of gastro-retentive floating microspheres using silymarin, curcumin and piperine for hepatoprotection

Misbah Sultana Abdul Kausar Badewale — 2025-08-31

Background: Curcumin, Silymarin, and Piperine are natural phytoconstituents with proven hepatoprotective effects; however, their therapeutic efficacy is limited by poor water solubility and low oral bioavailability. A gastro-retentive floating drug delivery system offers a strategic approach to enhance gastric residence time and improve absorption in the upper gastrointestinal tract. Methodology: Floating microspheres were developed using the solvent evaporation technique with Ethyl Cellulose and Eudragit RS 100 as polymers. A series of trial formulations was statistically optimized using Design Expert® software. The microspheres were evaluated for particle size, buoyancy, entrapment efficiency, drug release profile, and stability. Results and Discussion: The optimized formulation (Batch F3) demonstrated high encapsulation efficiency (>98%) and sustained buoyancy of 95.94% over 8-hour. At the end of 12 hours, cumulative drug release was 66.24% for Curcumin, 68.21% for Silymarin, and 72.82% for Piperine. Drug release followed zero-order kinetics, with the best model fit (R² = 0.9938) observed for Piperine. SEM images confirmed the presence of spherical and uniform microspheres. The formulation remained stable for 90 days under ICH Q1A(R2) conditions. Conclusion: The developed microspheres offer a promising gastroretentive system for controlled delivery of hepatoprotective agents, potentially improving therapeutic outcomes for liver-related disorders.

Formulation, optimization, and standardization of orodispersible herbal tablets using design of experiments (DOE)

Ganesh Shinde — 2025-08-31

Background: This study aimed to develop and optimize an orodispersible herbal tablet incorporating Achyranthes aspera Linn extract. Sodium Starch Glycolate and Crospovidone were employed as superdisintegrants to promote rapid tablet disintegration, while β-cyclodextrin was utilized to enhance the solubility of specific constituents within the extract. The optimized formulation exhibited a rapid disintegration time of 1.805 seconds and achieved a cumulative drug release of 98.04%, indicating improved dissolution and potential enhancement in oral bioavailability. Methodology: Orodispersible tablets were formulated using Design of Experiments (DOE) software, with crospovidone and sodium starch glycolate as independent variables, and time of disintegration and cumulative drug release as dependent variables. The formulation was evaluated for weight variation, uniformity, hardness, wetting time, and in vitro dispersion time. Result & Discussion: The optimized F6 batch of orodispersible herbal tablets demonstrated the following characteristics: hardness of 2.98 kg/cm², friability of 0.58%, weight variation of 3.319%, disintegration time of 13.805 seconds, wetting time of 34.4 seconds, content uniformity of 99.5%, water absorption of 36%, and cumulative drug release of 98.04%, all within the permissible limits as per official pharmacopoeialstandards. Conclusion: The study concludes that crospovidone and sodium starch glycolate effectively reduce disintegration time and improve cumulative drug release. These findings validate the reliability of the model, with minor deviations attributed to experimental variability.