Journal of Applied Pharmaceutical Research (JOAPR)
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Characterization and cytotoxicity evaluation of Ixora coccinea-derived iron oxide microparticles for biomedical applications
Get PDFBackground: This study aimed to synthesise and characterise iron oxide microparticles (IOMPs) using Ixora coccinea flower extracts and evaluate their antioxidant, anti-inflammatory, cytotoxic, and antidiabetic activities. Methodology: IOMPs were synthesised using Ixora coccinea flower extract and characterised using XRD, UV-Vis, EDAX APEX, and SEM. Bioactivity evaluations included anti-inflammatory and antioxidant activities via egg albumin, BSA, and DPPH assays; cytotoxicity through Brine Shrimp Lethality and zebrafish embryonic toxicity assays at 5, 10, 20, 40, and 80 μg/ml; and antidiabetic activity via alpha-amylase and alpha-glucosidase inhibition. Results: Fe₂O₃MPs demonstrated potent anti-inflammatory (83% protein denaturation inhibition at 50 μg/ml), antioxidant (94.26% inhibition at 50 μg/ml), and antidiabetic (86% α-amylase and 84% α-glucosidase inhibition at 50 μg/ml) properties, surpassing diclofenac sodium and ascorbic acid. Cytotoxicity tests revealed low toxicity, with LC50 values of 80.5 μg/ml (Brine Shrimp) and 82.4 μg/ml (zebrafish). Discussion: This study presents an eco-friendly synthesis of Fe₂O₃ microparticles using Ixora coccinea extract as a reducing and stabilising agent. These microparticles hold promise for biomedical applications, including drug delivery, MRI contrast enhancement, and hyperthermia treatment. Further research must optimise the synthesis process and assess the in vivo biocompatibility and therapeutic efficacy. Conclusion: This study addresses the need for eco-friendly nanoparticles. Conventional iron oxide microparticle synthesis uses toxic chemicals, but Ixora coccinea flower extract offers a sustainable alternative. Evaluating Fe₂O₃MPs' cytotoxicity and bioactivity provides insights into biomedical applications, supporting future investigations that link nanotechnology and therapeutics
Comparative phytochemical and antioxidative profiling of assamese culinary for developing antiarthritic polyherbal formulation
Get PDFBackground: Rheumatoid arthritis (RA) is a chronic inflammatory disorder where oxidative stress plays a critical role in disease progression with severe co-morbidities. Therefore, plant-derived bioactive compounds are increasingly explored due to their safety, affordability, and multi-targeted therapeutic properties. The present study aimed to comparatively evaluate four commonly used Assamese culinary herbs, Curcuma longa, Zingiber officinale, Piper nigrum, and Cinnamomum tamala for their phytochemical profile and antioxidant potential to identify candidates for synergistic anti-arthritic formulations. Methodology: Ethanolic extracts of the selected herbs were analyzed for TPC, TFC, and TTC using spectrophotometric assays, and bioactive constituents were identified via high-resolution LC-MS. Antioxidant activity was assessed using the DPPH and ABTS radical-scavenging assays. Data were statistically analyzed using one-way ANOVA followed by Tukey’s test (p<0.05). Result and Discussion: Among the tested herbs, turmeric showed markedly higher phytochemical content (TPC: 377.50±4.50 mg GAE/g, TFC: 294.29±2.18 mg CE/g, TTC: 201.25±3.14 mg TAE/g). HR-LCMS revealed characteristic compounds including curcumin (C. longa), 6-gingerol (Z. officinale), Dipiperamide E (P. nigrum), and eugenol (C. tamala). Antioxidant assays confirmed C. longa’s superior free-radical scavenging activity (DPPH IC50: 64.83±0.49 µg/ml; ABTS IC50: 145.60±0.95 µg/ml). Z. officinale, P. nigrum, and C. tamala extracts exhibited moderate but complementary activity profiles. Conclusion: The comparative phytochemical and antioxidant profiling demonstrated that C. longa was the most potent candidate, with Z. officinale, P. nigrum, and C. tamala exhibiting supportive bioactivity. The integrative evidence substantiated the rational design of synergistic polyherbal formulations targeting oxidative stress & inflammation in RA, with potential application in therapeutic development
Phytochemical profiling and in silico evaluation of Brassica oleracea stem bioactives as novel aldose reductase inhibitors for diabetic neuropathy treatment
Get PDFBackground: 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
Formulation, optimization, and standardization of orodispersible herbal tablets using design of experiments (DOE)
Get PDFBackground: 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
Scientific perspectives on Guillain-Barre Syndrome (GBS): A comprehensive review for sentience after early 2025 GBS outbreak in an Indian state
Get PDFBackground: 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
Pharmacognostical, phytochemical, and in vitro bioassay studies of Osbeckia stellata Buch-ham. leaves
Get PDFBackground: 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
Development and in vitro evaluation of liquid crystal-based polyherbal hair gels: physicochemical characterization, hair performance, and antioxidant assessment
Get PDFBackground: 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
Design, optimization, and antimicrobial assessment of Callicarpa longifolia-derived nanoparticles using quality by design (QbD) approach
Get PDFBackground: 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
Insilico molecular docking and ADME/T studies of flavonol compounds against selected proteins involved in inflammation mechanism
Get PDFBackground: Using computational tools in drug discovery advanced the research in identifying new drug candidates for the benefit of the pharmaceutical industry and assessing the safety and pharmacokinetic profiles of phytochemicals. Understanding the inflammatory mechanism is not possible, but inflammatory signal transduction by cytokines can be mitigated by using the flavonoid class of drugs like flavonols. Methodology: A molecular docking study of flavonol compounds with proteins linked with inflammation was carried out using the AutodockVina program. SwissADME and pkCSM modules were used to assess the pharmacokinetic features of plant products. Compared to commercially available NSAIDs, flavonols had more excellent molecular docking scores. Results: Calculation of ADME features of flavonols with no carcinogenicity and low oral acute toxicity level. Compared to anti-inflammatory medicines, the Rutin docking score against COX-I (-8.7 kcal/mol) and the Galangin docking score against COX-II enzymes (-9.4 kcal/mol) had higher values. Discussion: Molecular docking studies exhibited the highest docking score for COX-I is Rutin -8.7 Kcal/mol and hydrogen bond with THR-89, PRO-84, LS-468, GLY-471, PHE-470. The highest docking for COX-II is Galangin -9.4 Kcal/mol and hydrogen bonding with VAL-349 and TYR-385. ADME/T studies were performed for all the flavonols. Rutin has the highest violations in drug-likeliness studies. Conclusion: Flavonols may be more effective anti-inflammatory medicines than commercial medications. By modifying the pharmacokinetic features of plant products through diverse formulation strategies, we can get these phytochemicals to their target sites with fewer adverse effects
Investigation of molecular design, synthesis, and biological assessment of new benzopyran derivatives
Get PDFBackground: Tuberculosis (TB) remains a global health challenge, necessitating the discovery of novel anti-tubercular agents. The N-(8-hydrazinyl-3,4-dihydro-2H-1-benzopyran-6-yl)-N'-phenyl urea (HSM-II) scaffold has shown potential in developing effective drug candidates. Objective: This study aimed to design and evaluate 50 derivatives of HSM-II for their anti-tubercular activity, focusing on compounds demonstrating strong interactions with the protein PKS13 (PDB ID: 5v3y). Methods: A series of derivatives was synthesized, starting with the reaction of 8-bromo-3,4-dihydro-2H-1-benzopyran-6-amine and phenyl carbamic acid, yielding six new benzopyran derivatives. These were further treated with various aromatic halides to produce the HSM-II derivatives. Molecular docking studies were performed to identify compounds with high binding affinity to PKS13. Promising candidates (HSM-II-3, HSM-II-13, HSM-II-27, HSM-II-33, HSM-II-42, and HSM-II-49) were selected for biological evaluation. Anti-tubercular activity was assessed in vitro using the Alamar Blue Susceptibility Test (MABA) against Mycobacterium tuberculosis H37Rv and H37Ra strains. Results: Docking studies revealed high binding scores for the selected compounds, indicating strong interactions with the target protein. In vitro evaluations demonstrated significant anti-tubercular activity for the majority of synthesized derivatives. The pharmacologic profile of the compounds suggests potential as lead candidates for further optimization. Conclusion: This study presents the design, synthesis, and biological evaluation of 50 diverse derivatives of N-(8-hydrazinyl-3,4-dihydro-2H-1-benzopyran-6-yl)-N'-phenyl urea (HSM-II). Six derivatives (HSM-II-3, HSM-II-13, HSM-II-27, HSM-II-33, HSM-II-42, and HSM-II-49) demonstrated high binding affinities with PKS13 (PDB ID: 5v3y), with scores reaching -11.4 kcal/mol, and potent in vitro anti-tubercular activity, as assessed using the Alamar Blue Susceptibility Assay (MABA). Prominent derivatives exhibited MIC values significantly lower than those of standard drugs like rifampicin