Journal of Applied Pharmaceutical Research (JOAPR)
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Hot melt extrusion aided amorphous solid dispersions of quercetin and resveratrol for solubility enhancement
Get PDFBackground: 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
Formulation and optimization of upadacitinib-loaded transdermal patches for rheumatoid arthritis with zero-order release kinetics
Get PDFBackground: To develop and optimize Upadacitinib-loaded transdermal patches for rheumatoid arthritis treatment with improved patient compliance and sustained drug delivery. Methodology: Upadacitinib transdermal patches were formulated using a 3² factorial design approach with PVP K30 and HPMC K4M as key polymeric components. The patches were characterized for physicochemical, mechanical, and ex vivo permeation properties. Results and Discussion: The optimized formulation (SF8) exhibited excellent physicochemical characteristics, including high drug content (99.05 ± 0.83%), optimal mechanical properties with tensile strength of 0.912 kg/mm² and adhesion strength of 3.94 N. The ex vivo permeation reached 86.35% at 12h, with the flux of 102.91 μg/cm²/h following zero-order kinetics (R² = 0.9777). The experimental values closely matched predicted values with less than 2% error. Accelerated stability studies confirmed minimal changes in critical parameters over six months. Conclusion: The optimized Upadacitinib transdermal patch provides sustained drug delivery with zero-order release kinetics and excellent stability. This transdermal delivery system offers a promising alternative to oral therapy with potential advantages of improved patient compliance, reduced dosing frequency, and avoidance of first-pass metabolism for rheumatoid arthritis managemen
Biogenic zinc oxide nanoparticles from Saraca asoca: cytotoxicity, antioxidant, antimicrobial evaluation, and topical gel development
Get PDFBackground: Green synthesis of nanoparticles offers an eco-friendly and cost-effective alternative to conventional methods. Saraca asoca, a traditionally valued medicinal plant, contains bioactive compounds suitable for the fabrication of nanoparticles. This study reports the synthesis of zinc oxide nanoparticles (ZnO NPs) using Saraca asoca bark apozem and their incorporation into a biocompatible chitosan gel for topical applications. Methodology: ZnO NPs were synthesized via a green route using varying concentrations of zinc acetate (0.05–0.15 M) and Saraca asoca bark apozem (75–150 mg/mL), optimized through a 3² factorial design. The nanoparticles exhibited favorable formulation efficiency with % yield (40–46%), entrapment efficiency (55–62%), and drug loading (35–40%). Characterization confirmed nanoscale size (72.7–134.8 nm), negative zeta potential (–38.2 to –50.4 mV), UV–Vis absorbance (λmax = 366 nm), FTIR peaks of stabilizing –OH and –COO⁻ groups, and crystalline PXRD patterns. The optimized nanoparticles were incorporated into a 2% chitosan gel (Ash–ZnO NPs Cs gel). Results and Discussion: Antioxidant studies revealed strong free radical scavenging potential (IC₅₀ = 19.8 µg/mL). The Ash–ZnO NPs exhibited antimicrobial activity against Staphylococcus aureus and Candida albicans (MICs: 156.25 and 78.12 µg/mL). Cytotoxicity studies confirmed negligible toxicity (LC₅₀ > 1000 µg/mL). In vitro release studies demonstrated sustained and diffusion-controlled drug release, with Ash–ZnO NPs Cs gel achieving 96% release at 48 h compared to the burst release of silver nitrate gel. Conclusion: Saraca asoca-mediated ZnO NPs incorporated in chitosan gel represent a safe, stable, and multifunctional topical formulation. Their strong antioxidant, antimicrobial, biocompatible, and sustained release properties underscore their potential for wound healing and skin infection management
Formulation and optimization of metformin-berberine loaded solid lipid nanoparticles for their neuroprotective effects in the brain
Get PDFBackground: The increasing prevalence of Type 2 Diabetes Mellitus (T2DM) is associated with a heightened risk of developing Alzheimer’s Disease (AD), highlighting the need for effective therapeutic strategies that address the shared pathophysiological mechanisms in both conditions. Methodology: The Metformin-Berberine loaded solid lipid particles (MBSLNs) were prepared by dispersion of different concentrations of stearic acid, polysorbate 80, poloxamer 407, sesame oil, metformin, and berberine. Factor screening studies have been done to identify the influential components. An optimization study was then conducted using a three-factor Box-Behnken design with Design-Expert software. In-Vivo studies confirmed the neuroprotective role of SLNs. Results: The optimized concentrations of the variable factors were determined using the overlay plot generated by the software, resulting in stearic acid (4.84%), polysorbate 80 (1.50%), Poloxamer 407 (1%), and sesame oil (0.31%). The responses, particle size (10–200 nm), zeta potential (> ±30 mV), and polydispersity index (PDI) (0–1) were achieved within the desired range. Discussion: The closeness in experimental and predicted values confirms the reliability of the optimization technique. The optimized formulation exhibits a significant reduction in oxidative stress, and decreased glucose levels were observed when compared to the control, indicating a neuroprotective effect of the formulation. Conclusion: The optimized MBSLNs were affected by the independent parameters examined, including stearic acid, polysorbate 80, Poloxamer 407, and sesame oil concentrations, with significant effects on particle size, zeta potential, and size distribution. The utilization of MBSLNs has emerged as a remarkably effective strategy for enhancing the biological activity of Metformin and berberine in treating T2DM-induced AD
Formulation and evaluation of flucytosine-loaded nanoemulgel for enhanced antifungal activity through in vitro and in vivo studies
Get PDFBackground: Fungal skin infections constitute a prevalent global health issue, accompanied by increasing resistance to traditional antifungal medications. Flucytosine, a pyrimidine analogue exhibiting potent antifungal properties, is constrained in topical use due to inadequate skin absorption and fast elimination. Nanoemulgels, which integrate nanoemulsions with gels, enhance solubility, penetration, stability, and prolonged release, representing a viable approach for topical antifungal administration. Methods: The nanoemulgel was prepared utilizing Carbopol 940 as the gelling agent. The formulations (NEG1–NEG8) were evaluated for physical appearance, pH, viscosity, spreadability, drug content, and in vitro drug release and release kinetics. Antifungal activity was assessed by zone-of-inhibition assays and in vivo using Wistar rats infected with Candida albicans. Skin irritation, histopathology, and a three-month stability study were also conducted. Result and Discussion: The improved NEG5 formulation had a favorable pH (5.92±0.03), high drug content (95.3±1.83%), and maximum cumulative drug release (92.97±5.91% at 24 hours) with first-order release kinetics (R2= 0.9959). The commercial luliconazole cream and NEG5 showed increased antifungal effectiveness in vivo, with lesion clearance by Day 14. The histopathology showed tissue repair with minimal inflammation. NEG5 surpassed other formulations in zone-of-inhibition assays for antifungal activity. No skin irritation was reported, and the formulation was stable for three months under various storage conditions. The improved physicochemical and therapeutic performance of NEG5 suggests enhanced skin penetration and sustained drug release, addressing the limitations of conventional flucytosine therapies. Conclusion: Flucytosine-loaded nanoemulgel (NEG5) offers a promising, effective topical treatment for fungal skin infections with improved drug delivery and patient safety
A review on the structure, distribution, and biological activities of biflavonoids in clusiaceae
Get PDFBackground: The Clusiaceae family is widely distributed in tropical and subtropical climates, with a rich source of structurally diverse metabolites. Among these, biflavonoids stand out due to their complex structures and significant pharmacological activities. This review aims to examine data on various Clusiacean biflavonoids, their structural diversity, and bioactivity, thereby increasing the understanding of their implications in both traditional and modern medicine. Methodology: Data were collected from electronic databases like PubMed, Elsevier, Springer, and Google Scholar. The structural categorization of biflavonoids was based on the nature of linkage and substituent variations that influence their biological activities. Their distribution across Clusiacean members further highlights their chemotaxonomic importance. Additionally, structure-activity relationship studies reveal that specific linkages and functional groups enhance biological activity. Results and Discussion: Studies indicate that Clusiacean biflavonoids are potential candidates for drug discovery and therapeutic development due to their varied pharmacological activities. Approximately 21 biflavonoids from Clusiacean members are included in this review; nine of them exhibit antioxidant, five antimicrobial, five early antigen inhibition, four monoamine oxidase inhibition, three anti-inflammatory, three neuromuscular transmission inhibition, one antidiabetic, one anti-aging, and one hypocholesterolemic activity. Conclusion: Clusiacean biflavonoids possess desirable compounds for drug development owing to their diverse pharmacological activities, including antiviral, anti-inflammatory, anti-cancer, antioxidant, and neuroprotective properties, and so on. Overall, this article analyzes different biflavonoids obtained from Clusiaceae species, focusing on their structural diversity, biological importance, and structure-activity relationships
Gastroprotective potential of Dolichandrone falcata extract via modulation of oxidative stress, inflammation, and mucosal healing
Get PDFBackground: Dolichandrone falcata, traditionally used for gastrointestinal disorders, has demonstrated antiulcer activity, but the underlying protective mechanisms remain unclear. This study evaluated the methanolic extract of D. falcata for gastroprotective, antioxidant, and anti-inflammatory activities using ethanol- and pylorus-ligation–induced ulcer models in rats. Methodology: Wistar rats were divided into control, standard, and treatment groups. Ulcers were induced by ethanol or pyloric ligation. The extract (100, 200, and 400 mg/kg) and omeprazole (20 mg/kg) were administered orally. Ulcer index, gastric parameters, oxidative stress markers [malondialdehyde (MDA), glutathione (GSH), superoxide dismutase (SOD), catalase (CAT)], and inflammatory cytokines [TNF-α, IL-6] were assessed, supported by histopathological examination. Results and Discussion: The extract produced a dose-dependent reduction in the ulcer index in both models, with 76.6% protection at 400 mg/kg, comparable to omeprazole (79.7%). Histology revealed marked restoration of the gastric mucosa with minimal necrosis. MDA levels decreased significantly, while GSH, SOD, and CAT levels were elevated toward normal. TNF-α and IL-6 were markedly suppressed, indicating a reduction in oxidative and inflammatory injury. Conclusion: D. falcata extract demonstrated potent gastroprotective effects through antioxidative, anti-inflammatory, and mucosal-healing mechanisms. This is the first biochemical and cytokine-based validation of its traditional use, suggesting strong potential for developing D. falcata as a plant-derived therapeutic for ulcer management
A comprehensive review on the applications of chemometrics in analytical chemistry
Get PDFBackground: This article presents a review of the various applications of chemometrics in analytical chemistry. Chemometrics is essential to analytical chemistry because it provides sophisticated methods for extracting, analyzing, and interpreting chemical data. To maximize analytical procedures, enhance data reliability, and extract insights, this field combines statistical and mathematical techniques with chemical research. Chemometrics provides analytical chemists with the means to manage the massive datasets generated by contemporary analytical methods, such as spectroscopy and chromatography. Methodology: This review combines data from previous research articles that have elaborated and described the various applications of chemometrics in the analytical chemistry sector. Results and Discussion: The combination of chemometrics with artificial intelligence and machine learning offers more advanced analytical and predictive modelling possibilities. It is anticipated that these developments will transform analytical chemistry by enhancing researchers' ability to manage complex datasets and gain deeper insights from their investigations. This is especially important in industries where precise data interpretation is critical, such as pharmaceuticals, ecological surveillance, and food safety. Conclusion: Chemometrics is essential to contemporary analytical chemistry because it provides methods and instruments that enhance quality control, facilitate innovative research advancements, and improve data analysis capabilities. The accuracy and efficacy of chemical analyses are expected to continue to improve as this sector develops
Spectrophotometric methods for determination of naringin, amlodipine, and nifedipine using chemometric techniques
Get PDFBackground: Chemometrics articulates statistical and mathematical aspects to analyse the effectiveness of chemical data, playing a pivotal role in spectroscopy. Among all the chemometrics techniques, this study utilizes the Orthogonal partial least squares (OPLS) model for the simultaneous analysis of naringin, amlodipine, and nifedipine, a well-established calcium channel blocker. Naringin, a citrus flavonoid exhibiting notable pharmacological activities. Methodology: This research employs UV-visible spectrophotometry in conjunction with the OPLS method for both calibration and prediction sets in simultaneous studies of Amlodipine–Naringin and Nifedipine–Naringin, aiming to develop a precise model for measuring drug concentrations. A linear dynamic range of 5-20 µg/mL was achieved for standard solutions, while calibration sets were developed using factorial designs. Result and Discussion: The OPLS model had significant predictive performance with R2 values within the range of 0.9947-0.9976 for calibration and 0.9947-0.9985 for prediction, and low root mean square error of cross validation (RMSECV) values of 0.6191- 0.4353 for NIF-NAR, and 0.3978- 0.4418 for AML-NAR, indicating robust model performance. The model validation process, using Hotelling’s T2 test, DModx, established no significant outliers, and permutation analysis validated the model’s reliable fit. The recovery studies showed values close to 100%, thus verifying the effectiveness of the methodology. Conclusion: The research demonstrated OPLS (Orthogonal Partial Least Squares) as a powerful solution for resolving overlapping spectral data, providing high-precision drug analysis with minimal interference. The development of chemometrics methods demonstrated efficiency and precision in pharmaceutical analysis while also offering cost-effectiveness for quality control and formulation development
RP-HPLC method for quantitative estimation of naftifine hydrochloride in formulated products: development and validation
Get PDFBackground: 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