Journal of Applied Pharmaceutical Research (JOAPR)
Not a member yet
396 research outputs found
Sort by
QbD-guided HPTLC method development and validation for quantitative estimation of anticancer drugs
Get PDFBackground: Olaparib, Abiraterone acetate, and Pazopanib are critical anticancer agents used in the treatment of breast/ovarian, prostate, and renal cancers, respectively. Ensuring their quality through precise, cost-effective analytical techniques is vital for routine quality control (QC). Given their clinical importance, a robust method capable of quantifying these drugs individually and indicating their stability under stress is highly desirable. Methodology: High-performance thin-layer chromatography (HPTLC) methods were developed for each drug, guided by a Quality by Design (QbD) approach. A 2³ factorial design was employed to optimize three critical method parameters: mobile phase composition, chamber saturation time, and detection wavelength. Chromatographic analysis was performed on aluminum-backed silica gel plates with detection wavelengths set at 278 nm (Olaparib), 255 nm (Abiraterone acetate), and 254 nm (Pazopanib). Method validation followed ICH Q2(R2) guidelines, assessing linearity, accuracy, precision, LOD/LOQ, specificity, and robustness. Forced degradation under acidic, basic, oxidative, thermal, and photolytic conditions was evaluated to assess the stability-indicating capability. Results and Discussion: All methods exhibited strong linearity (r² > 0.997), high accuracy (98–102% recovery), and precision (%RSD < 2). Sensitivity was excellent, with LOD as low as 28 ng/spot for Olaparib. Under stress, degradation ranged from 5% to 20%, with distinct degradant peaks and peak purity indices of> 0.995, confirming no co-elution and indicating stability. The validated methods were successfully applied to stressed marketed formulations. Conclusion: The QbD-optimized HPTLC methods are accurate, economical, and stability-indicating, making them suitable for routine QC of Olaparib, Abiraterone acetate, and Pazopanib in pharmaceutical dosage forms
Design, characterization, and evaluation of an aceclofenac cocrystal for improved solubility and stability
Get PDFBackground: Co-crystallization enhances APIs by forming noncovalent interactions with coformers, thereby improving physicochemical properties. Aceclofenac was selected for its low solubility, whereas L-lysine serves as a coformer to enhance solubility and stability via hydrogen bonding. This strategy effectively improves the solubility, stability, and bioavailability of poorly soluble drugs. Methods: The aceclofenac–lysine co-crystal was synthesized using the Neat Grinding technique. The synthesized cocrystal was characterized by powder X-ray diffraction (PXRD), differential scanning calorimetry (DSC), Hot stage microscopy (HSM), and Fourier transform infrared spectroscopy (FTIR). Dissolution behavior, stability, and in vivo anti-inflammatory activity were evaluated in comparison with pure aceclofenac. Results: PXRD and DSC confirmed a new crystalline phase, while FTIR revealed hydrogen bonding between aceclofenac and lysine. The cocrystal exhibited a 2.66-fold improvement in dissolution (91.84% vs. 34.41% at 90 min) and superior stability, maintaining >86% dissolution after six months at 40°C/75% RH, compared to ~30% for pure aceclofenac. In vivo studies demonstrated enhanced anti-inflammatory efficacy, with 81.50% edema inhibition versus 74.35% with the pure drug (p < 0.0001). Discussion: The ACF-lysine cocrystal achieved dissolution enhancement that maintained stability over six months, and demonstrated statistically significant improvement in anti-inflammatory efficacy, confirming superior therapeutic performance over pure aceclofenac. Conclusion: Co-crystallization with L-lysine effectively enhanced aceclofenac's biopharmaceutical and pharmacological performance. The aceclofenac-lysine co-crystal exhibited 2.66-fold faster dissolution, greater stability under accelerated storage, and significantly improved anti-inflammatory efficacy (81.50% vs. 74.35% edema inhibition; p < 0.0001) compared with pure aceclofenac. These results demonstrate the value of amino acid coformers in improving the solubility of poorly soluble drugs
Assessment of pharmacognostical, physiochemical, and in-vitro anti-inflammatory potential of S. cordata
Get PDFBackground: The current study aimed to investigate the pharmacognostical, physiochemical, and anti-inflammatory potential of Sida cordata. In this study, macroscopic, microscopic, and physicochemical analyses were performed. Methodology: This medicinal plant, commonly used in traditional medicine, was evaluated using the in vitro albumin denaturation method. The study aimed to assess the plant's ability to inhibit protein denaturation, a critical factor in the inflammatory process. The water extract and acetic acid extract of Sida cordata were tested at various concentrations (10, 50, 100, 150, 200, 250 µg/ml), and the results indicated a dose-dependent inhibition of albumin denaturation. Result & Discussion: The rate of inhibition of egg albumin denaturation for water extract (WE) is 86.55±0.63, and acetic acid extract (AAE) is 82.18±1.43. The maximum inhibition observed was compared with the standard anti-inflammatory drug (diclofenac sodium). Conclusion: These findings suggest that the water and acetic acid extracts of Sida cordata possess significant anti-inflammatory activity, supporting its traditional use as a remedy for inflammatory conditions
Evaluation of a polyherbal formulation in gastric ulcer models induced by naproxen and acetic acid in Wistar Rats
Get PDFBackground: Gastric ulcers remain a prevalent gastrointestinal disorder, often exacerbated by non-steroidal anti-inflammatory drugs (NSAIDs) like Naproxen and irritants such as acetic acid. The investigation focuses on evaluating the gastroprotective properties of a formulation composed of standardized extracts from traditionally used medicinal plants, evaluated in Wistar rat models with experimentally induced gastric ulcers. Methodology: Ulcers were induced using Naproxen (NSAID-induced model) and acetic acid (chronic ulcer model) to mimic acute and chronic ulcerative conditions. The polyherbal formulation was administered orally at graded doses prior to ulcer induction. Ulcer index, gastric volume, pH, and histopathological parameters were assessed to determine protective effects. Results: The polyherbal formulation significantly reduced ulcer index in a dose-dependent manner, with the highest dose (1180 mg/kg) lowering the index to 0.44 ± 0.02 in Naproxen-induced ulcers (67.45% protection) and to 2.21 ± 0.01 in acetic acid-induced ulcers (61.25% protection), closely approaching omeprazole’s efficacy. Discussion: The formulation demonstrated a significant reduction in ulcer index and improved gastric mucosal integrity, with notable restoration of antioxidant defense mechanisms. Histological studies revealed reduced mucosal damage and inflammation compared to control groups. Conclusion: These outcomes recommend that the polyherbal formulation utilizes a protective effect against gastric ulcers, likely through cytoprotective, anti-inflammatory, and antioxidant mechanisms. The study supports the therapeutic potential of polyherbal combinations in managing gastric ulcers and encourages further clinical investigation
Antimicrobial activity of bioactive compounds extracted from Chara globularis Thuill
Get PDFBackground: The algae, a vastly diversified group of species on Earth, offer numerous benefits to humanity. Chara globularis is one such green alga that contains potential bioactive compounds. Methodology: This current study investigates the antifungal and antibacterial potential of Chara globularis extracts obtained using methanol, acetone, and hexane solvents, along with their phytochemical and medicinal profiles. Results & discussion: The antifungal activity was evaluated against clinically significant fungal strains, including Microsporum gypsum, Trichophyton rubrum, and T. mentagrophytes. The methanol extracts exhibited the most potent inhibition zones, with T. rubrum showing a maximum inhibition of 24 mm at a concentration of 4 mg. Also, antibacterial assays against pathogens such as Staphylococcus aureus, Escherichia coli, and Klebsiella pneumoniae demonstrated strong activity, especially in methanol and acetone extracts at higher concentrations. Comparative control studies using fluconazole and tetracycline confirmed the efficacy of the extracts, suggesting potential for pharmaceutical application. GC-MS analysis of the methanol extract identified 26 bioactive compounds, notably pentadecanoic acid and eicosatrienoic acid, which possess antimicrobial, anti-inflammatory, and cardioprotective properties. Conclusion: Nutrient profiling further revealed high levels of essential macro and micronutrients, highlighting the nutritional value of Chara globularis. The findings support the plant’s potential as a natural source of therapeutic agents with broad-spectrum antimicrobial and nutraceutical applications
Evaluation of the melanin synthesis-inhibitory potential of Morus alba L. leaf extract for the development of a natural anti-hyperpigmentation formulation
Get PDFBackground: Although Morus alba (white mulberry) has long been used in traditional skin care, the scientific evidence for its leaf extract in anti-hyperpigmentation applications remains limited, particularly regarding its incorporation into topical formulations. This study investigated the melanin-synthesis-inhibitory, tyrosinase-inhibitory, and antioxidant activities of M. alba leaf extract and evaluated its potential in a stable topical gel formulation. Methodology: Melanin suppression was assessed in IBMX-stimulated B16F10 melanocytes using microscopic observation, pellet analysis, and quantitative melanin measurement. Tyrosinase inhibition was examined with a mushroom tyrosinase assay, while antioxidant capacity was evaluated via DPPH radical scavenging. A topical gel containing M. alba extract was developed and assessed for physicochemical properties, phenolic retention, bioactivity, and stability. Result and Discussion: The extract showed strong tyrosinase inhibition (IC₅₀ = 5.70 ± 0.28 µg/mL) and antioxidant activity (IC₅₀ = 16.22 ± 0.6 µg/mL), and significantly reduced melanin synthesis in B16F10 cells without cytotoxicity (≤ 200 µg/mL). The formulated gel maintained phenolic content, exhibited moderate tyrosinase inhibition, and demonstrated stable appearance, pH, spreadability, and bioactivity during storage. Conclusion: Morus alba leaf extract possesses potent anti-melanogenic and antioxidant properties and can be successfully incorporated into a stable topical gel, supporting its potential as a natural ingredient for anti-hyperpigmentation products. However, these findings are based on in vitro assays and preliminary formulation studies; further in vivo and clinical evaluations are needed to confirm its efficacy and safety in humans
Development and validation of a robust QbD-guided (RP-HPLC) analytical technique for quantifying coenzyme Q10 in pharmaceutical dosage form
Get PDFBackground: Coenzyme Q10 (CoQ10) is a lipophilic antioxidant that contributes to mitochondrial energy production but poses analytical challenges due to low solubility and oxidative sensitivity. An accurate and validated method is essential to ensure quality control of its pharmaceutical dosage forms. Methodology: A reverse-phase high-performance liquid chromatography (RP-HPLC) method was designed using Quality by Design (QbD) principles. A Central Composite Design was employed to study the influence of critical parameters, including flow rate, gradient time, and mobile phase ratio. Separation was carried out on a Gemini C18 column (250 × 4.6 mm, 5 µm) with gradient elution using ethyl acetate: acetonitrile (50:50) and methanol: acetonitrile (80:20) containing 0.1% ammonia. The method was validated in accordance with ICH-Q2 (R1) guidelines. Results: The optimized conditions yielded a sharp CoQ10 peak at approximately 12.9 minutes with high resolution (Rs > 36), theoretical plates (~33,800), and acceptable tailing (≤1.3). Linearity was established over 2.5–200 µg/mL (r² = 0.9997). Accuracy ranged from 99.2–101.4%, precision was within %RSD ≤1.5%, and robustness was demonstrated under deliberate variations. Discussion: The method proved capable of consistently quantifying CoQ10 with superior specificity and sensitivity. Application to commercial soft gel formulations confirmed assay values at 99.5% of the label claim, meeting pharmacopeial standards. Conclusion: This QbD-based RP-HPLC method offers a validated, reproducible, and regulation-compliant strategy for the quality control and stability assessment of CoQ10 dosage forms, with potential extension to similar pharmaceutical compounds
Nanostructured lipid carriers (NLCs): A comprehensive review of drug delivery advancements
Get PDFBackground: Nano-structured lipid carriers (NLCs) have emerged as a significant advancement in lipid-based drug delivery systems. Compared to Solid Lipid Nanoparticles (SLNs), NLCs offer improved drug loading capacity, stability, and controlled release profiles. Objective: This review article explores the structural and functional benefits of NLCs, their enhanced bioavailability, and their potential in targeted therapeutic agent delivery. Methodology: We investigated the unique combination of solid and liquid lipids in NLCs, which creates an internal structure for improved drug encapsulation and sustained release. Various methods were analyzed for their contribution to NLC efficacy, including high-pressure homogenization and solvent emulsification. Results and Discussion: NLCs demonstrated encapsulation efficiency ranging from 85–95%, with particle sizes between 100–300 nm. Drug release was sustained over 24 hours, affirming their effectiveness in controlled drug delivery. Applications of NLCs were highlighted across diverse delivery modes, including topical, pulmonary, oral, parenteral, and ocular. Challenges such as scaling production, overcoming biological barriers, and ensuring regulatory compliance were also addressed. Conclusion: NLCs present a promising future in pharmaceutical sciences, with the potential to improve therapeutic outcomes in complex diseases like cancer and neurodegenerative disorders. Continued research into NLC formulations is critical for advancing patient outcomes and addressing global health challenges
Exploring 1,3,4-oxadiazole derivatives for hepatocellular carcinoma: synthesis, and bioactivity evaluation
Get PDFBackground: Cancer is a leading cause of death globally, with existing treatments often limited by resistance and toxicity. This necessitates the development of new, more effective anticancer therapies.
Methodology: This study used In-silico modeling with tools like Pre-ADMET and Molinspiration to evaluate the physicochemical, pharmacokinetic, and pharmacodynamic properties of substituted 1,3,4-Oxadiazole derivatives. Results and discussion: Computational studies of 1,3,4-Oxadiazole analogues showed promising drug-like properties and bioavailability. To test the inhibitory efficacy against the protein target tyrosine kinase (PDB: 1M17), 30 designed derivative compounds underwent molecular docking experiments. 10 synthesized derivatives were structurally confirmed through Mass, NMR, and IR spectrometry, ensuring their purity and identity. Molecular docking and in vitro tests identified compound S23 as a potent tyrosine kinase inhibitor, with significant anti-proliferative activity (GI50: 0.25665634) and enzyme inhibition (IC50: 1.87), highlighting its potential as a therapeutic agent. Conclusion: According to our findings, the substituted derivative might offer superior potential for developing anticancer medicine
HR-LCMS based metabolites profiling, pharmacognostic study, and antimycotic activity of leaves of Ruellia asperula
Get PDFBackground: 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 therapie