Background: Enhanced utilization of certain drugs may be possible through the development of alternative delivery forms. It has been observed that NSAIDs have adverse gastrointestinal tract effects such as irritation and ulceration during anti-inflammatory therapy. This challenge may be overcome through nano topical formulations.
Objective: This study aimed to explore the potentials of a transdermal nanovesicular formulation for safe and enhanced delivery of piroxicam (PRX), a poorly water-soluble NSAID.
Methods: Preformulation studies were conducted using DSC and FTIR. Ethosomal nanovesicular carrier (ENVC) was prepared by thin-film deposition technique using Phospholipon® 90 H (P90H) and ethanol and then converted into gel form. The formulation was characterized using a commercial PRX gel as control. Permeation studies were conducted using rat skin and Franz diffusion cell. Samples were assayed spectrophotometrically, and the obtained data was analyzed by ANOVA using GraphPad Prism software.
Results: The preformulation studies showed compatibility between PRX and P90H. Spherical vesicles of mean size 343.1 ± 5.9 nm, and polydispersity index 0.510 were produced, which remained stable for over 2 years. The optimized formulation (PE30) exhibited pseudoplastic flow, indicating good consistency. The rate of permeation increased with time in the following order: PE30 > Commercial, with significant difference (p< 0.05). It also showed higher inhibition of inflammation (71.92 ± 9.67%) than the reference (64.12 ± 7.92%).
Conclusion: ENVC gel of PRX was formulated. It showed potentials for enhanced transdermal delivery and anti-inflammatory activity relative to the reference. This may be further developed as a safe alternative to the oral form.
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http://dx.doi.org/10.2174/2211738509666210129151844 | DOI Listing |
Int J Pharm
January 2025
College of Engineering, Virginia Commonwealth University, 601 West Main Street, Richmond, VA 23284, USA. Electronic address:
Intranasal drug administration offers a promising strategy for delivering combination antiretroviral therapy (cART) directly to the central nervous system to treat NeuroAIDS, leveraging the nose-to-brain route to bypass the blood-brain barrier. However, challenges such as enzymatic degradation in the nasal mucosa, low permeability, and mucociliary clearance within the nasal cavity must first be addressed to make this route feasible. To overcome these barriers, this study developed solid lipid nanoparticles (SLNs) with varying PEGylation levels (0 %, 5 %, 10 %, and 15 % w/w of PEGylated lipid), co-encapsulated with Elvitegravir (EVG) and Atazanavir (ATZ) as an integrase and protease inhibitor, respectively.
View Article and Find Full Text PDFMol Pharm
January 2025
Institute of Chinese Medical Sciences (ICMS), State Key Laboratory of Quality Research in Chinese Medicine, University of Macau, Macau 999078, China.
The Biopharmaceutics Classification System (BCS) has facilitated biowaivers and played a significant role in enhancing drug regulation and development efficiency. However, the productivity of measuring the key discriminative properties of BCS, solubility and permeability, still requires improvement, limiting high-throughput applications of BCS, which is essential for evaluating drug candidate developability and guiding formulation decisions in the early stages of drug development. In recent years, advancements in machine learning (ML) and molecular characterization have revealed the potential of quantitative structure-performance relationships (QSPR) for rapid and accurate BCS classification.
View Article and Find Full Text PDFPharmaceutics
October 2024
Department of Pharmaceutics and Industrial Pharmacy, Cairo University, Cairo 11562, Egypt.
The lack of local availability for drugs in the colon can be addressed by preparing a self-microemulsifying drug delivery system (SMEDDS) of curcumin (Cur) which is ultimately used for the treatment of inflammatory bowel disease (IBD). From preformulation studies, Lauroglycol FCC (oil), Tween 80 (surfactant), Transcutol HP (co-surfactant), and Avicel (solid carrier) were selected for the preparation of blank liquid and solid Cur-loaded SMEDDSs (S-Cur-SMEDDSs). Z-average size (12.
View Article and Find Full Text PDFMaterials (Basel)
November 2024
Section of Pharmaceutical Technology, Department of Pharmacy, School of Health Sciences, National and Kapodistrian University of Athens, Panepistimioupolis Zografou, 15771 Athens, Greece.
The aim of the present study is to evaluate the stability of DMPC:Pluronic F-127 and DPPC:Pluronic F-127 liposomes, both with and without incorporated quercetin. Quercetin belongs to the class of flavonoids and has shown antioxidant, antiviral, anti-inflammatory, anti-cancer, and antimicrobial activities. Dynamic light scattering, electrophoretic light scattering, and differential scanning calorimetry (DSC) were utilized to investigate the cooperative behavior between liposomal components and its effect on stability.
View Article and Find Full Text PDFInt J Pharm
January 2025
Faculty of Pharmacy, Alamein International University, Alamein 51718, Matrouh, Egypt. Electronic address:
This study aimed at preparing sustained release rosuvastatin (Ru) calcium carbonate (CC) co-precipitate nano-formulation for local intra-osseous application in osteoporotic rats. Nano-formulations were prepared by the co-precipitation method using different concentrations of polyvinyl alcohol (PVA) (0.2, 0.
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