Journal of Applied Pharmaceutical Research (JOAPR)
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Fabrication and study of release kinetics of moxifloxacin and dexamethasone loaded nanostructured lipid carrier system for ocular drug delivery
Get PDFBackground: The combination of moxifloxacin hydrochloride (MOX) and dexamethasone sodium phosphate (DEX) is widely available in the conventional commercial market for treating ocular infections and inflammations. Traditional ocular delivery systems are inferior to nanostructured lipid carriers (NLCs) due to their poor drug bioavailability, rapid tear drainage, and limited drug penetration. In contrast, NLCs offer sustained release, enhanced corneal absorption, and improved drug stability. Thus, the research aims to develop moxifloxacin and dexamethasone-loaded NLC for effective drug release. Methodology: In this study, a combination of MOX and DEX drugs was loaded in an NLC. The NLC was prepared using standard methods and evaluated for characteristic properties, including particle size (PS), polydispersity index (PDI), entrapment efficiency (EE), and drug loading (DL), as well as drug encapsulation and in vitro studies. Results and Discussion: The optimized formulation of NLC possessed a particle size of 190.58 nm and a polydispersity index of 26.7%. The fabricated drug exhibited a KP model release kinetics, indicating that drug release occurred via a combination of diffusion and polymer reaction. The NLC also exhibited a PDI of 26.7%, indicating a moderately uniform particle size distribution, which further suggests a consistent particle size, an acceptable characteristic for nano-carrier systems. The FT-IR analysis revealed optimal encapsulation of drugs inside the lipids, thereby achieving the desired objectives of drug fabrication. Conclusion: The formulated NLC has a particle size that falls within the ideal range for a smooth surface in commercial NLC formulations. Additionally, the prepared NLCs' adherence to the KP model underscores their potential as an advanced drug delivery system
Novel microwave-assisted solid dispersion technology enhances piroxicam dissolution and therapeutic efficacy: an in vitro and in vivo study
Get PDFBackground: 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
A paradigm shift in bioavailability enhancement using solid self emulisifying drug delivery system
Get PDFBackground: 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
Designing a sustained-release solid oral formulation for overactive bladder treatment: a quality by design approach
Get PDFBackground: 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
Get PDFBackground: 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
Identification of novel potential benzimidazole derivatives by pharmacophore generation, 3D-QSAR, virtual screening, molecular docking and ADME/ TOX analysis against breast cancer as targeted estrogen alpha receptor
Get PDFBackground: The estrogen alpha receptor (ERα) is critical in breast carcinogenesis. Although selective estrogen receptor modulators like tamoxifen are clinically used, their adverse effects highlight the need for safer alternatives. The study uses computational methods to identify potential ERα inhibitors within a benzimidazole scaffold. Methodology: This study employed computational approaches, including pharmacophore generation, 3D-QSAR, virtual screening, molecular docking, and in silico ADME/Tox analysis. The best pharmacophore model (DDRRR_1) identified two hydrogen donors and three aromatic rings as critical features. Moreover, a rigorous external validation was used on decoy databases with optimized metrics (ROC, BEDROC, AUROC). A subsequent atom-based 3D-QSAR model with a high correlation coefficient (R² = 0.9), cross-validated coefficient (Q² = 0.8), and Fisher ratio (F = 80.1) was developed. Benzimidazole scaffolds from PubChem were screened, followed by docking against ERα (PDB ID: 3ERT) and ADMET profiling. Results and Discussion: The pharmacophore model validated the importance of the identified features. The 3D-QSAR model effectively screened benzimidazole scaffolds, with five component PLS factors, supporting the pharmacophore findings. This model effectively screened benzimidazole scaffolds obtained from the PubChem database, followed by molecular docking against the targeted protein ERα (PDB ID: 3ERT) and identified five promising compounds. ADME/Tox profiling revealed PubChem ID 3074802 (2-[2-(1H-indol-3-yl) ethyl]1H-benzimidazole) has favourable pharmacokinetics and a low toxicity profile. Conclusion: These findings indicate that PubChem ID 3074802 is a promising candidate for further therapeutic drug development in breast cancer treatment. It demonstrates the highest binding affinity (-9.842 kcal/mol) compared to the standard drug Tamoxifen (-5.357 kcal/mol) and exhibits a favorable ADME/Tox profile
A mechanism-driven strategy for in-silico prediction, molecular docking, synthesis, and biological assessment of substituted 1,3,4-oxadiazole derivatives as novel antidiabetic agents
Get PDFBackground: Diabetes mellitus is a long-standing and debilitating metabolic condition that imposes a substantial global health burden, leading to severe and widespread complications. Objectives: This study aims to predict physicochemical properties of 1,3,4-oxadiazole derivatives using in-silico methods and molecular docking simulations to explore their potential as α-glucosidase inhibitors for diabetes management. Furthermore, this study aims to experimentally synthesize and characterize these derivatives to validate their inhibitory activity. Methods: In silico drug-likeness, pharmacokinetic, and toxicity profiling of substituted oxadiazole derivatives were performed using the Molinspiration and PreADMET web tools. Molecular docking simulations were conducted with the target protein alpha-glucosidase (PDB ID: 3WY1) to assess its anti-diabetic potential. This study suggests that oxadiazole has the potential to be a novel anti-diabetic agent. Results: Compound 3a1 formed 5 significant hydrogen bonds with Gly228, Thr226, Leu227, Tyr235, Glu271 with docking scores of -156.118 and re-rank scores of -91.600 comparable to the standard drug Miglitol, which formed 6 hydrogen bonds Val380, Asp401, Lys398, Gly399, Glu377, Asp379 but had lower docking and re-rank scores (-69.4415 and -95.887). Based on docking results, five oxadiazole derivatives were synthesized via Mannich base cyclization, yielding 62.2 – 79.9%. They showed moderate to excellent anti-diabetic activity, with compounds 3a1 and 3a3 demonstrating no toxicity or mortality at 40 mg/kg oral dose. Conclusion: Our study highlights that the oxadiazole pharmacophore is a key structural motif for the development of potential anti-diabetic compound
A review on the bioactive compounds of Rhus chinensis Mill. native to the Sikkim Himalayas
Get PDFBackground: The Sikkim Himalaya is home to the wild medicinal shrub Rhus chinensis Mill, which produces edible fruits. Traditionally, the fruit juice concentrate has been used to treat a variety of stomach issues. The plant is rich in phytoconstituents, including gallic acid (up to 130.4 ± 2.5 mg/g), methyl gallate, flavonoids, and tannins, which contribute to its traditional applications in managing conditions such as diarrhoea, dysentery, toothache, cough, and wounds. The total flavonoids and flavonol levels were quantified as rutin equivalents. The total phenolics were calculated as gallic acid equivalents. Through various in vitro antioxidant methods, including DPPH, Total antioxidant content, ABTS, and Hydrogen peroxide scavenging assays, the antioxidant capacity was determined. Methodology: This review combines data from numerous research studies and review articles that have elaborated on the various phytoconstituents, medicinal uses, and pharmacological properties of different Rhus species. Results and Discussion: This review provides a detailed description of multiple phytoconstituents, traditional uses, and medicinal applications of Rhus species. The quantitative findings from previous studies report the total phenolic content as 123.52±1.29 mg GAE/g. IC50 values through DPPH free radical scavenging assay and Hydrogen scavenging assay were 42.69±0.1% and 63.20±1.48% respectively. Conclusion: This review provides an in-depth description of various phytoconstituents, including gallic acid, citric acid, myricetin-3-O-rhamnoside, methyl gallate, quercetin-3-O-arabinoside, and protocatechuic acid, among others. These results provide concrete evidence to support the potential of Rhus chinensis Mill. as a source of bioactive compounds for the creation of new treatments
Formulation and evaluation of curcumin coated central venous catheters in the eradication of catheter-related blood stream infections
Get PDFBackground: Biofilm formation on catheters after implantation, leading to the development of catheter-related bloodstream infections, is a significant concern with the usage of vascular catheters, leading to the death of hospitalized patients. The research aimed to modify the catheter surface by developing a coating technique using PU, PVP, and curcumin. Methodology: A dip coating technique with a base coat of PU and a top coat of PVP was used on 7 French triple-lumen Polyurethane CVCs with the antimicrobial agent Curcumin. Based on the concentration of polyurethane used, 5 formulations were prepared and evaluated as per ISO guidelines. Results and Discussion: Dip coating was successful in coating the catheters. All the physical parameters were within the ISO limits. The process parameters that produce uniform coating were studied. The coated catheters were radiopaque. At the end of 24 hours, all formulations displayed an initial burst release due to the top coat of PVP. Formulation E demonstrated a sustained release of 94.17% of the drug over 21 days. The amount of polyurethane included in the base coat determines how long the sustained release lasts. The formulation follows zero-order kinetics and fits the Higuchi model with quasi-Fickian release, indicating that the release is diffusion-controlled. Conclusion: The dip coating technique proved to be a successful method for developing drug-coated central venous catheters. Coating with curcumin reduces bacterial colonization, growth on the catheter surface, and biofilm formation, thereby preventing CRBSI, which in turn enhances patient outcomes and lowers healthcare expenses
Development and validation of stability indicating RP-HPLC method for nebivolol by using the DOE approach
Get PDFBackground: Nebivolol (NBV), classified as a third-generation β1-adrenergic receptor antagonist, is commonly prescribed for managing hypertension. Accurate and prompt quantification of NBV in bulk materials and pharmaceutical formulations is crucial for quality assurance. This research focuses on developing and validating a stability-indicating RP-HPLC method for the quantification of NBV, with an emphasis on sensitivity, precision, accuracy, and robustness. Methodology: A stability-indicating reversed-phase high-performance liquid chromatography (RP-HPLC) method was established using an Agilent 1260 Infinity II HPLC system equipped with a Diode Array Detector (DAD). The chromatographic analysis was conducted on an Agilent Zorbax Bonus RP column (250 × 4.6 mm, 5 µm). The mobile phase comprised acetonitrile and 0.1% perchloric acid in a 55:45 (v/v) ratio, delivered at a flow rate of 1 mL/min. Detection was performed at a wavelength of 282 nm. The method underwent validation according to the guidelines provided by the International Council for Harmonisation (ICH), including assessments of linearity, precision, accuracy, robustness, and forced degradation studies. Results and Discussion: This method demonstrated improved sensitivity, shorter run time (retention time of 4.22 min), and high precision. Forced degradation studies confirmed Nebivolol’s instability under alkaline (15.94%) and oxidative (8.57%) conditions, highlighting the method’s stability-indicating capability. The method also gives robust linearity across the concentration range of 80–120 µg/mL, with a correlation coefficient (r²) of 1.00. The limits of detection (LOD) and quantification (LOQ) were determined to be 0.55 µg/mL and 1.61 µg/mL, respectively. Conclusion: The proposed RP-HPLC method proved to be reliable, precise, and stability-indicating, making it a valuable tool for the quality control and stability assessment of Nebivolol formulations in pharmaceutical settings