Journal of Applied Pharmaceutical Research

New information on the etiology and biological targets of wounds associated with diabetes

Niladry S. Ghosh, Anubhav Dubey, Mamta Kumari — Fri, 28 Feb 2025 00:00:00 -0500

Background: Wound healing is a complex process that advances through inflammation, proliferation, and remodelling phases. Diabetes precipitates numerous ailments that obstruct practically all of these reparative processes. Methodology: We performed a literature search on ScienceDirect and PubMed databases using various keywords, including "Diabetes Wound Healing." The search was refined by applying relevant filters to obtain the most pertinent articles for this review article's objective. Results: Patients with diabetes may incur wounds during or after medical interventions. The wound healing process comprises remodelling, proliferation, and inflammation. Diabetes impedes nearly all of these healing processes through various pathological changes. This study primarily examines the molecular pathways of inflammatory substances, including growth stimulants and other factors that hinder wound healing. It also examines molecular targets and the current advancements in wound care and complete healing. Conclusion: Based on our investigation, we identified several practical approaches for treating wound inflammation and proposed that combining these strategies may yield the most significant results in our research domain.

A paradigm shift in bioavailability enhancement using solid self emulisifying drug delivery system

Sankararajan Umadevi, Rajathi Senthil Boopathi, Ezhilarasan — Fri, 28 Feb 2025 00:00:00 -0500

Background: Solids are physically and chemically more stable compared to liquid formulations. The Solid SEDDS form is preferred over the liquid SEDDS form to enhance the oral bioavailability of lipophilic medications. Solid SEDDS are isotropic mixtures of oil, surfactant, and co-solvent. Methodology: A liquid-solid compact approach is followed to convert liquid SEDDS into solid SEDDS. Melt granulation, melt extrusion, spray drying, adsorption to solid carriers, and freeze drying are some approaches to converting liquid SEDDS into solid SEDDS. Various solid self-emulsifying materials in several solid dosage forms, like solid dispersions, tablets, capsules, and powders. Result and discussion: Solid SEDDS results in solubility studies, particle size and polydispersity index (PDI), zeta potential, in vitro drug release, solid-state characterization (e.g., XRD, DSC), and stability studies. In summary, S-SEDDS seems to be a viable strategy for improving the distribution of poorly water-soluble drugs through enhanced bioavailability, stability, and administration simplicity. Conclusion: In this review, the research will be extended to the different approaches toward improving the bioavailability, stability, and solubility of poorly soluble drugs into solid SEDDS. All these components are intended to act as primary instructions for future development in SSEDDS.

Hot melt extrusion aided amorphous solid dispersions of quercetin and resveratrol for solubility enhancement

Lakshmi Swapna Sai, Fatima S Dasankoppa, Srinivas Mutalik, Muralidhar Pisay — Fri, 28 Feb 2025 00:00:00 -0500

Background: Conversion of poorly soluble drugs into amorphous solid dispersions using different carriers is a formulation approach to improve solubility. Objective: The study investigates hot melt extrusion as an approach for producing amorphous solid dispersions that contribute to solubility enhancement. Methodology: Solid dispersions were hot melt extruded using two model compounds – quercetin and resveratrol with different carriers. The resulting solid dispersions were analyzed for solubility enhancement and characterized by various techniques. Results and Discussion: The solubility of solid dispersions was evaluated, revealing a 36-fold increase in the solubility of quercetin from 0.023 mg/ml to 0.823 mg/ml and a 97-fold increase in the solubility of resveratrol from 0.053 mg/ml to 5.125 mg/ml with soluplus as a carrier. Various characterization studies indicated the conversion of crystalline forms of quercetin and resveratrol into their amorphous forms, which was confirmed by powder x-ray crystallographic and scanning electron microscopic studies. In addition, the particle size reduction of quercetin reduced from 1.53 μm to 0.48 μm and resveratrol of 10.26 μm particle size was reduced to 0.22 μm in solid dispersions with soluplus as the carrier with decreased polydispersity index. Conclusion: This research demonstrates hot melt extrusion as a practical approach for fabricating amorphous solid dispersions.

Exploring the structural aspects of alanine racemase enzyme for antitubercular drug discovery – a computational approach

Unni Jayaram, Parthan Anilkumar, Fathima Rifana Yousuf, Graceson Jose — Fri, 28 Feb 2025 00:00:00 -0500

Background: Tuberculosis (TB) is a communicable disease that is a significant cause of ill health and one of the leading causes of death worldwide. The current antibiotics have been pivotal in managing TB to a greater extent. Still, the issue of antitubercular drug resistance is indeed a matter of concern and requires effective drug discovery strategies targeting less explored targets. One of the less explored but promising antitubercular targets, Alanine racemase (AlaR), a prokaryotic enzyme providing the essential peptidoglycan precursor D-alanine (D-Ala) in bacterial cell wall synthesis, is an attractive target for antitubercular drug discovery. Objective: The current study aims to explore the available protein targets of the AlaR enzyme in Mycobacterium tuberculosis and to understand the structural aspects to be followed in designing inhibitors for them. Methodology: As a part of the study, the crystal structure of the alanine racemase enzyme from Mycobacterium tuberculosis was subjected to computational studies using the Schrodinger drug design suite. The significant protocols followed involved protein preparation and fragment-based drug design studies. Results and discussion: The in-silico data suggested that substituted pteridine derivatives, which impart stable interaction at the active site of the alanine racemase enzyme, may be the potential lead moiety for drug design. Conclusion: Although the preliminary screening suggests that the pteridine ring system may be a promising lead, detailed in silico studies must be carried out, such as molecular mechanic generalized born surface area (MM-GBSA), density functional theory (DFT) studies, induced fit docking, molecular dynamics, etc. for further authentication. For effective correlation, detailed in vivo studies on AlaR enzyme inhibition can be carried out from a future perspective.

Novel microwave-assisted solid dispersion technology enhances piroxicam dissolution and therapeutic efficacy: an in vitro and in vivo study

Charit Kumar, Arun Nanda — Fri, 28 Feb 2025 00:00:00 -0500

Background: Piroxicam (PRX), a nonsteroidal anti-inflammatory drug, exhibits poor aqueous solubility, limiting its therapeutic efficacy. Enhancing solubility can directly improve bioavailability and therapeutic effectiveness. This study explores the development of a new solid dispersion (SD) system of PRX using polyvinylpyrrolidone (PVP K30) as a carrier by MW-assisted method. Methods: The involvement of microwave (MW) in the solvent evaporation method is a newer concept aimed at enhancing the solubility and in vivo bioavailability of PRX. Various ratios of PRX: PVPK30 (1:5, 1:7, 1:9, and 1:11 w/w) were evaluated using conventional and MW-assisted solvent evaporation methods and conducted in vitro dissolution studies. Results: The optimized MW-assisted formulation (1:7 w/w) exhibited 94.69±0.24% drug release in 15 minutes, showing a 5.37-fold increase compared to pure PRX (17.63%) and surpassing the marketed drug release (90.82±0.39%). Fourier Transform Infrared, Differential Scanning Calorimetry, Thermogravimetric analysis, Scanning Electron Microscopy, and powdered X-ray diffraction authenticated the OF. In vivo studies demonstrated significant enhancements (p<0.0001) compared to control. The anti-inflammatory activity showed increased paw oedema inhibition (44.4±0.4%) compared to control and pure PRX (35.37±0.3%). The analgesic activity of OF demonstrated improved pain response time (10.6±0.8 seconds) compared to control (4.2±0.5 seconds) and pure PRX (8.1±0.7 seconds). Conclusion: The SD developed via the MW-assisted drug formulation technique significantly enhances the solubility, bioavailability, and therapeutic efficacy of PRX, offering a potential strategy to improve clinical outcomes for similar drugs with solubility challenges.

Novel coumarin chalcone derivatives: synthesis, docking, and antimicrobial evaluation

Sumita Kumari, Amit Sharma, Sonia Yadav — Fri, 28 Feb 2025 00:00:00 -0500

Background: This study synthesized and evaluated a series of coumarin chalcones for their antimicrobial efficacy against microbial and fungal strains. Methodology: Ten new coumarin chalcones were prepared by Claisen- Schmidt condensation by using 4-hydroxy coumarin as a precursor and followed by refluxing obtained intermediate (3-(4-aminophenyl)-3-oxo prop-1-enyl)-4-hydroxy-2H-chromen-one) with substituted aromatic benzaldehyde in the presence of piperidine as a catalyst. IR, 1HNMR, 13CNMR, and GCMS characterized all synthesized compounds. The agar well diffusion method assessed these compounds for antimicrobial activity against various bacterial and fungal strains such as E. coli, P. aeruginosa, B. subtills, S. aureus, and C. albicans. Zone inhibition was measured for each compound (10µL) against all strains. Results and Discussion: The study showed that derivatives 4c, 4e, 4f, and 4g showed strong potential for inhibition towards various fungal and microbial strains. The inhibition zone for 4c and 4e was emerged as 5.48±0.448, 7.02±0.332, 5.62±0.321, 6.81±0.021, 7.72±0.421 and 5.13±0.179, 6.76±0.511, 4.24±0.273, 4.64±0.231, 5.48±0.049 while compound 4f and 4g showed 5.40±0.420, 6.69±0.168, 5.71±0.245, 5.28±0.042, 7.09±0.175, and 4.94±0.814, 6.58±.0160, 6.01±0.455, 6.61±0.021, 6.91±0.414 mm, respectively. Between -7.1 to -10.2Kcal/mol is the range of docking score of derivatives by interactions of DNA gyrase and compounds analyzed. Here, compound 4g exhibited the highest DNA gyrase inhibition, and compound 4c exhibited a strong inhibition with docking scores of -10.2 kcal/mol and -9.8 kcal/mol, respectively. Conclusion: The findings of this work contribute to a better understanding the potential of synthesised compounds as drug candidate against microbial infections through ADMET study.

Exploring key compounds in callicarpa longifolia: a study on isolation and identification

Md. Shakeel Alam, Nidhi Shrivastava — Fri, 28 Feb 2025 00:00:00 -0500

Background: The present study aims to extract the bioactive phyto-components from the hydroalcoholic extract of Callicarpa longifolia. The study also aims to isolate and characterize the phytochemicals through quantitative and qualitative measures. Methodology: The mixture of Toluene, Ethyl Acetate, and Acetic Acid (8:4:0.4) was used as a solvent system with the thin-layer chromatography (TLC) technique. Twelve distinct spots were observed, indicating the presence of a variety of compounds with Rf values ranging from 0.12 to 0.89. The specific fractions were isolated using silica gel column chromatography, which was further analyzed with TLC. Results and Discussion: Fraction F showed consistency with standard terpenoids and was subjected to advanced analytical techniques for further evaluation. UV-visible spectroscopy identified a key absorption peak at 288 nm, while Fourier-transform infrared (FTIR) spectroscopy revealed functional groups such as alcohols, hydroxyls, alkanes, alkenes, and carboxylic acids. The compound's structure and proton environment were confirmed through ^1H Nuclear Magnetic Resonance (NMR) spectroscopy. The compound was identified as Methyl 3,11-dioxo-olean-12-en-28-oate with the molecular formula C₃₁H₄₆O₄, supported by mass spectrometry (M+ peak at 482.33 m/z). Conclusion: The significant bioactive terpenoids identified in the C. longifolia hydroalcoholic extract highlight its potential for developing therapeutic agents, particularly for anti-inflammatory and anticancer applications. The detailed phytochemical characterization provides a robust foundation for future studies exploring the pharmacological and clinical applications of C. longifolia. Quantitative analysis and advanced spectroscopic techniques confirmed the compound's identity and established its importance in medicinal chemistry.

Investigation of molecular design, synthesis, and biological assessment of new benzopyran derivatives

Fri, 28 Feb 2025 00:00:00 -0500

Background: 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.

Insilico molecular docking and ADME/T studies of flavonol compounds against selected proteins involved in inflammation mechanism

Narendra Pentu, Ajitha Azhakesan, Pasupuleti Kishore Kumar — Fri, 28 Feb 2025 00:00:00 -0500

Background: 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.

Novel RP-HPLC method development and validation for precise quantification of prochlorperazine maleate in pharmaceutical dosage forms

Nikhil Shrisunder, Prashant Kumar Dhakad, Ritu Gilhotra — Fri, 28 Feb 2025 00:00:00 -0500

Background: Prochlorperazine Maleate, a piperazine phenothiazine derivative, exhibits strong antiemetic and antipsychotic properties. However, existing analytical methods for its quantification in pharmaceutical formulations often face limitations regarding sensitivity, specificity, and accuracy. Many conventional techniques involve extensive sample preparation and prolonged analysis times, making them less feasible for high-throughput quality control. This study developed and validated a novel, precise, and highly sensitive reverse-phase high-performance liquid chromatography (RP-HPLC) method for Prochlorperazine Maleate quantification to overcome these challenges. Methodology: An RP-HPLC method was established using an Agilent Zorbax Bonus-RP column (250 × 4.6 mm, 5 µm) with a mobile phase of 0.1% formic acid and acetonitrile (70:30). The detection was performed at 258 nm using a diode array detector. Method validation followed ICH guidelines, assessing linearity, precision, accuracy, robustness, and sensitivity across a 100–150 µg/mL concentration range. Results and Discussion: The method displayed strong linearity (R² = 0.999). The LOD and LOQ were 1.76 µg/mL and 5.35 µg/mL, respectively. High precision (%RSD < 2%) and recovery rates (99–101%) confirmed accuracy. Robustness was established through consistent retention time and peak symmetry. Conclusion: This validated RP-HPLC method is reliable, sensitive, and cost-effective, making it ideal for routine pharmaceutical quality control and future stability studies.

Designing a sustained-release solid oral formulation for overactive bladder treatment: a quality by design approach

Neeraj Sharma, Daksh Bhatia, Sharda Shambhakar, Pavitra Solanki — Fri, 28 Feb 2025 00:00:00 -0500

Background: Mirabegron, a first-in-class β3-adrenergic agonist used for managing overactive bladder (OAB), is well-documented in the literature. However, its low oral permeability results in poor bioavailability, limiting patient compliance and tolerability. To address this, the present study focuses on developing a sustained-release (SR) tablet of mirabegron with enhanced oral effectiveness. In this research, mirabegron was combined with polyethylene oxide to improve permeability and formulated as an HPC-loaded SR tablet, promising improved bioavailability and anti-OAB efficacy. Methods: Tablet design and optimization were carried out using the Box-Behnken Design (Design Expert® 12 software) to refine formulation parameters. The study aimed to create a commercially viable SR tablet with improved intestinal permeability, bioavailability, and clinical acceptance. Results: The optimized formulation showed a 34.8% increase in bioavailability compared to the marketed tablet. In vivo pharmacokinetic studies demonstrated a 31.77% increase in plasma concentration over the marketed formulation. Conclusion: The developed formulation is safe and effective, offering improved therapeutic potential for treating overactive bladder. This work represents a significant advancement in OAB management and highlights the commercial viability of the emerging mirabegron SR tablet in meeting current therapeutic needs.

Isolation and characterization of cellulose derived from prominent agricultural waste (Sugarcane bagasse) and its utilization in various biomedical field

Fri, 28 Feb 2025 00:00:00 -0500

Background: Agricultural waste clearance and reutilization is a significant problem today. Objective: Successful extraction and purification of cellulose and its derivatives (methylcellulose) from agri-waste and pollution. This is an innovative polymer (cellulose & its derivatives) that can be used in pharmaceutical and technical applications in an eco-friendly manner. Aim: Isolate and characterize cellulose derived from prominent agricultural waste (sugarcane bagasse) and its utilization in various biomedical fields. Method: Eco-friendly Soxhlet extraction utilizing organic solvents was employed to give a high yield of cellulose. Further, the obtained cellulose was bleached and transformed into ester derivatives, such as methylcellulose, to analyze their properties. Result: This study’s primary goal is to concentrate on the production of cellulose and its extraction from different agricultural waste & its characterization. The cellulose isolated from different biomass was comparatively evaluated for its varied properties and was found suitable for use in the pharmaceutical industry or technical dimensions. Conclusion: Agri waste has significant potential and sources for value-based products. Here, successful extraction and derivatization of the cellulose from the sugarcane were done. These extracted celluloses were further subjected to various pharmacopeial, micromeritics, and physiochemical properties assessments, including advanced characterization to evaluate and validate the properties of the products, which signifies more efficient, green extraction and pharmacopeial utilization.

HR-LCMS based metabolites profiling, pharmacognostic study, and antimycotic activity of leaves of Ruellia asperula

Arshu Patel, J R Kudnar, R S Jadhav, B Ghuge — Fri, 28 Feb 2025 00:00:00 -0500

Background: Fungal infections pose a global health challenge, exacerbated by rising drug resistance and immunocompromised populations. Ruellia asperula, a traditional medicinal plant, has garnered attention for its bioactive compounds, including flavonoids and alkaloids. This study aims to profile its metabolites using HR-LCMS and evaluate its antimycotic potential, contributing to the discovery of natural therapeutic agents. Methodology: Leaves and bark of Ruellia asperula were collected, authenticated, and processed for analysis. Physicochemical standards like moisture content, ash values, and extractive yields were determined. Preliminary phytochemical screening identified bioactive compounds. Ethanolic extracts were prepared via Soxhlet extraction, fractionated through column chromatography, and analyzed using HR-LCMS. In vitro, antimycotic assays were conducted against Alternaria and Macrophomia. Results: Physicochemical analysis revealed a total ash content of 2.87% w/w, water-soluble ash of 25.78% w/w, and alcohol-soluble extractive value of 9.53% w/w, indicating substantial secondary metabolites. Phytochemical screening identified alkaloids, flavonoids, and saponins. HR-LCMS analysis detected 18 compounds in the ethanolic fraction and 13 in the chloroform fraction. In vitro assays demonstrated significant inhibition of Alternaria and Macrophomia, with activity comparable to Itraconazole. Discussion: Ruellia asperula leaves demonstrated high phytochemical quality and are rich in flavonoids and alkaloids. HR-LCMS profiling identified bioactive metabolites, while in vitro tests confirmed significant antifungal activity. These findings underscore the plant's potential as a natural antimycotic agent. Conclusion: This study highlights the phytochemical richness of Ruellia asperula, confirmed by HR-LCMS and pharmacognostic analyses. Its potent antimycotic activity, comparable to Itraconazole, positions it as a promising candidate for natural fungal therapies

Ethnobotanical survey of medicinal plants for bone fracture treatment in Lingmoo, Sikkim

Bhumika Chettri, Tiewlasubon Uriah Khar, Sonam Bhutia — Fri, 28 Feb 2025 00:00:00 -0500

Background: This study documents the use of herbal plants by traditional healers in Lingmoo, Namchi district, Sikkim, to treat bone fractures. Methodology: The methodology used were survey-based, pre-structured questionnaire, field investigation and face to face interaction with one traditional healer. We have recorded about 29 ethno-medicinal plants naturally available in the selected area. Results: According to the survey results, a total of 29 numbers of ethnomedicinal plant species belonging to 23 different families (Rosaceae topped the list) were identified and summarized in Table 1. The study revealed that herbs (48%) are mainly used, followed by trees (24%), climbers (17%), and shrubs (11%). In case of frequency of use, these plants were highly cited during the interview: rivularis, Kaempferia rotunda, Viscum articulatum, Urtica dioica, Curcuma longa, Lepidium sativum, Beaumontia grandiflora, Bergenia ciliate, and Laportea bulbifera. The parts used were roots, stem barks, whole plants, and seeds. The most commonly used preparation was paste. According to gender-wise comparison, males (60%), females (25%), and children (15%) were getting the treatment. Out of 29 plant species, 12 species are abundant and, 1 is in threatened condition; only 3 species are cultivated in present days. Conclusion: Documentation of local plants used by a specific traditional healer will benefit the sustainable use of indigenous medicinal plant practices. It will also provide preliminary information for future biological resource management and research development, which will eventually help in the conservation of ethnomedicinal plants and the advancement of such ideas.

Fabrication of levofloxacin-loaded ph-sensitive eudragit polymeric floating microballoon biomaterial for gastroretentive drug delivery

Manivasakam Prakash, Venkateswaramurthy Nallasamy, Senthil Venkatachalam — Fri, 28 Feb 2025 00:00:00 -0500

Background: The design of improved biomaterials for medication administration is vital in overcoming problems associated with standard therapy for Helicobacter pylori (H. pylori)-induced stomach ulcers. This study aims to develop and characterize floating biomaterial of levofloxacin microballoon biomaterials based on a fluoroquinolone-benzoxazine system conjugated with methylated piperazine and carboxylic acid groups, strategically designed for prolonged gastric delivery. Methodology: Using the emulsion solvent diffusion method, thirteen preparations were developed by different polymer ratios (pH-sensitive Eudragit RS-100 and Ethyl Cellulose), stirring speeds, and temperatures. Results and Discussion: In the buoyancy study simulated gastric fluid (pH 1.2), the best formulation (F9) shows superior encapsulation efficiency (90.2%) and sustained drug release profile (91.2% over 8 hours) that increases its effectiveness against H. pylori. FTIR and SEM analyses conducted during characterization studies verified the drug stability and the spherical microballoon morphology, with a particle size of 81.2 µm. Levofloxacin-loaded microballoon biomaterials provide a unique gastro-retentive delivery system that improves patient compliance, reduces off-target effects, and maintains effective drug concentrations at the infection site, thereby strengthening the therapeutic efficacy of levofloxacin against H. pylori. Conclusion: This creative method offers a viable substitute for traditional therapies for stomach ulcers and is consistent with the overarching objectives of targeted delivery systems and structure-based drug development.

Characterization and cytotoxicity evaluation of Ixora coccinea-derived iron oxide microparticles for biomedical applications

Fri, 28 Feb 2025 00:00:00 -0500

Background: 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.

Enhancement of flow properties, solubility, and dissolution of the atazanavir by spherical crystallization

Ashok T Jadhav, Sanjay S. Pekamwar — Fri, 28 Feb 2025 00:00:00 -0500

Background: The present work aimed to develop spherical agglomerates of Atazanavir (ATZR) with enhanced flow properties, compressibility, solubility, and dissolution. 2² full factorial design approach was employed to develop agglomerates. Methodology: ATZR spherical agglomerates were prepared using bridging solvent Benzene, methanol, HPMC and evaluation for different properties. Then, ATZR immediate release (IR) capsules were formulated using spherical agglomerate, wet granulation, and direct compaction methods. Results and discussion: The spherical agglomerates resulted in a significant enhancement of micromeritic properties. The drug content was ranged from 91.9 % (SAA6) to 97% (SAA2). Drug content and solubility (4.88 to 39.89 mg/ml) were directly related to the concentration of HPMC and inversely related to benzene concentration (p<0.05). Nearly 10.12-fold enhancement in solubility of ATZR was found with spherical agglomerates. FTIR analysis demonstrated excellent compatibility between the drug and the polymer. XRD results indicated the amorphization of pure ATZR during agglomeration. The agglomerates exhibited spherical particle morphology. DSC analysis confirmed the effective encapsulation of the drug. Nearly 100% release was observed within 10 minutes from the F1 capsule formulation containing ATZR spherical agglomerates. Conclusion: The optimized SAA2 spherical agglomerates were utilized to manufacture immediate-release capsules via direct filling (F1). Spherical agglomerates significantly enhanced the flow properties and compressibility of the blend compared to pure ATZR. Drug release from the F1 batch was notably faster than F2 and F3 formulations. The study demonstrates the substantial improvement in flow properties, compressibility, solubility, and dissolution of ATZR using spherical agglomerates.