Journal of Applied Pharmaceutical Research (JOAPR)
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New information on the etiology and biological targets of wounds associated with diabetes
Get PDFBackground: 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
QbD enabled optimization study of the variable concentration of phospholipid and stabilizer in the development of liposomal pastilles of solid dispersion polymeric composite of antihypertensive drug
Get PDFBackground: The study aimed to develop and optimize liposomes of the antihypertensive drug Felodipine (FH) using the Quality by Design (QbD) approach with a 3² Central Composite Design (CCD) in Design Expert software, followed by the development of pastilles. Methodology: Liposomes were prepared using the solvent injection method, with soya lecithin and cholesterol as key excipients, and a solid dispersion of FH. The impact of their concentrations on particle size (PS), drug content (DC), entrapment efficiency (EE), and in vitro and ex vivo drug release was analyzed using response surface methodology. The optimized formulation was validated using four batches (optimized batch, VC1, VC2, and VC3), ensuring a minimal percentage error. The liposomal formulation was incorporated into pastilles to enhance patient compliance, and these were evaluated for drug content, dissolution, bioadhesion, and stability. Results and Discussion: The optimized liposomes exhibited desirable properties, including a positive surface charge (PS, 1.41±0.12), a high DC (94.323±1.03), a high EE (69.61±1.13), in vitro drug release (70.73±1.08), and ex vivo drug release (66.88±0.23). The validation batches showed minimal percentage error, confirming the optimization process. The pastilles demonstrated excellent physical stability and bioadhesion, indicating their potential for improved patient compliance. Conclusion: The study showed the effectiveness of the QbD approach in optimizing a liposomal drug delivery system for FH, thereby minimizing the need for extensive trials. The incorporation of liposomes into pastilles provided a patient-friendly dosage form with enhanced bioadhesion and stability, making it a promising alternative for antihypertensive drug delivery
Protective effect of peonidin - anthocyanidin class flavonoid against doxorubicin-induced toxicity in H9C2 cardiomyoblast cell lines
Get PDFBackground: This study investigates the cardioprotective properties of peonidin against cytotoxicity induced by doxorubicin (DOX) in H9c2 cardiomyocytes using both in vitro and in silico methods. H9c2 cells were exposed to DOX alone as well as in combination with different concentrations of peonidin for various time durations. Methodology: Cytoprotection was studied using MTT assay for viability, LDH leakage, SOD activity, lipid peroxidation, and ROS content. Furthermore, molecular docking was also performed to analyze the binding affinity of peonidin with angiotensin-converting enzyme (ACE) and endothelin-converting enzyme-1 (ECE-1), utilizing captopril as a control. Results and Discussion: DOX drastically inhibited cell viability, whereas peonidin co-treatment maintained it dose dependently, restoring it to 99.74% at 150 µg/mL after 72 h. LDH release through DOX-triggered membrane disruption was alleviated from 175.84% to 78.40% by peonidin. ROS levels were also decreased from 191.13% (DOX) to 61.29% by peonidin, reflecting robust antioxidant activity. Lipid peroxidation was strongly inhibited, and SOD activity, decreased by DOX (36.59±0.306 AU), was restored close to control levels (97.85±0.313 AU) by peonidin. Docking studies indicated that peonidin exhibited a superior binding affinity with ACE (-95.72 kcal/mol) and ECE-1 (-78.08 kcal/mol) compared to captopril, characterized by good van der Waals and hydrogen bonding interactions. Conclusion: Peonidin potently mitigates DOX-induced oxidative injury in cardiomyocytes, showing great promise as a natural cardioprotective agent, as evidenced by both biochemical assays and molecular docking studies against ACE and ECE-1
Mechanical and dissolution properties of Eudragit L100 and S100 films in buffer solutions
Get PDFBackground: 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
Development of a stability-indicating UPLC method for quantification of mirvetuximab soravtansine-gynx in pharmaceutical formulations using quality by design (QbD) principles
Get PDFBackground: This study intended to introduce a robust ultra-performance liquid chromatography (UPLC) method for quantifying Mirvetuximab soravtansine-gynx (MSG) in pharmaceutical dosage forms. A systematic approach incorporating the Design of Experiments (DoE) was employed to optimize reliable, sensitive, and efficient chromatographic conditions. Methodology: The finalized method utilized a Waters ACQUITY BEH Phenyl (50 mm) Column with a mobile phase comprising acetonitrile and 0.1% aqueous formic acid in 30:70 (v/v) at 0.2 mL/min and 271 nm and PDA wavelength. Results and discussion: The method validation demonstrates excellent linearity (R² = 0.991, p < 0.05) over 17.50–105 µg/mL. The Intraday and interday precision (%RSD) values were 0.568 and 0.544, respectively, confirming method reproducibility. Accuracy was validated through recovery studies, which produced results within the range of 100.1–100.5%, whereas the robustness test highlights the method's resilience to minor variations. This method detects MSG at a very low concentration of 0.42 µg/mL, confirming method sensitivity. The forced degradation studies were conducted under various stress conditions. The result suggests that moderate degradation of 10.3%, 14.5%, and 9.5 % was noticed in acidic, peroxide, and reduction (9.5%) conditions. Conclusion: The purity analyses confirm the absence of significant impurities in the stress degradation chromatogram, highlighting the stability of MSG and the reliability of the proposed method. In conclusion, the proposed method was rapid, sensitive, precise, robust, and stable for quantifying MSG in pharmaceutical formulations
Development and characterisation of lyophilised ethambutol-loaded polymeric nanoparticles
Get PDFBackground: Tuberculosis (TB) remains a universal health crisis, requiring innovative drug delivery systems to overcome challenges like prolonged treatment duration and patient non-adherence. This study was designed to develop Ethambutol (ETH)-loaded poly-ε-caprolactone (PCL) nanoparticles (NPs) as a sustained-release pulmonary delivery platform for TB therapy. Methodology: ETH-PCL NPs were fabricated using the nanoprecipitation technique with Lutrol® F68 as a stabiliser. The formulation was optimised for physicochemical properties (particle size, polydispersity index (PDI), zeta potential), encapsulation efficiency (EE), and morphology (SEM). In vitro drug release and 3-month colloidal stability were evaluated. Results and Discussion: The optimised NPs exhibited a rod-shaped morphology with smooth surfaces, an average size of 426.3 ± 13.03 nm, PDI < 0.467, zeta potential of -18.8 ± 0.520 mV, and EE of 76.57±3.86%. Sustained ETH release (86.62% over 24 h) and robust colloidal stability (negligible changes in size, PDI, and zeta potential over 3 months) were achieved. The formulation's biodegradable PCL core and scalable design align with the need for cost-effective, patient-centric therapies. Conclusion: ETH-PCL NPs represent a promising nanocarrier platform for TB, combining sustained drug release, high encapsulation efficiency, and long-term stability. While in vitro results are encouraging, future studies must validate in vivo efficacy and pulmonary delivery potential. This work underscores the viability of nanotechnology in addressing TB treatment challenges, particularly in improving adherence and targeting mycobacteria-laden macrophages
Novel RP-HPLC method development and validation for precise quantification of prochlorperazine maleate in pharmaceutical dosage forms
Get PDFBackground: 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
A systematic review of Alzheimer's disease: exploring genetic and environmental risk factors, biomarkers, and future pharmacotherapy for cognitive decline and neurodegeneration
Get PDFBackground: Alzheimer's disease (AD) is the most prevalent form of dementia, affecting millions globally through progressive cognitive decline caused by neurodegeneration in cholinergic brain regions. Aging is the primary risk factor, but metabolic, genetic, and environmental influences, including inflammation and vascular dysfunction, significantly contribute to disease onset and progression. Methodology: This comprehensive review evaluates diagnostic methods, biomarkers, and genetic and environmental risk factors associated with AD, focusing on recent advancements (2022–2025). The study selection process prioritized clinical trials, systematic reviews, and meta-analyses related to AD pathophysiology, diagnostics, and therapeutic interventions while excluding research with ambiguous findings or lacking methodological rigor. A PRISMA flowchart illustrates the study selection process, ensuring transparency. Pharmaceutical and non-pharmacological interventions, along with multi-target therapeutic strategies, were critically analyzed. Results and Discussion: AD pathology is driven by amyloid-beta plaques and tau tangles, leading to synaptic dysfunction and neurodegeneration. Current treatments, including acetylcholinesterase inhibitors and NMDA receptor antagonists, offer symptomatic relief but are ineffective in halting disease progression. Emerging therapies such as monoclonal antibodies (Lecanemab, Donanemab), tau inhibitors, and neuroinflammation modulators show potential in slowing cognitive decline and preserving neuronal health. Advances in biomarker-based diagnostics (e.g., p-tau217) and AI-powered precision medicine have improved early detection and personalized treatment strategies, though challenges in cost, accessibility, and regulatory approval persist. Conclusion: A multisystem approach combining pharmacotherapy, biomarker-driven diagnostics, and AI-assisted personalized medicine is essential to optimize AD treatment effectiveness. Future research should focus on developing innovative, multidisciplinary treatment strategies to enhance patient outcomes and quality of life
Transdermal delivery of risedronate using chemical enhancers for improved skin penetration
Get PDFBackground: 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
A QbD-based stability-indicating RP-HPLC method for larotrectinib: degradation kinetics and integrated white, green, and blue analytical assessment
Get PDFBackground: 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