Mefenamic acid (MA) has been reported as a weakly soluble drug which presents weak absorption upon oral administration using conventional formulations. Solid dispersions (SDs) have been investigated extensively in literature for enhancing the solubility and bioavailability of weakly-soluble molecules. Hence, the aim of proposed study was to prepare MA novel formulations in the form of SDs using hot-melt extrusion technology in order to enhance its palatability, bioavailability, and pharmacodynamics effects/anti-inflammatory efficacy. Various SDs of MA were prepared using hot-melt extrusion technology, characterized physically and investigated for dissolution tests. Optimized SD formulations of MA were being subjected to palatability, pharmacodynamics, and pharmacokinetic studies in rats. Optimized SD of MA showed significant rat palatability tastes as compared with pure and marketed MA ( < .05). Anti-inflammatory efficacy of 20% SD and 25% SD of MA was found to be 86.44 and 89.83%, respectively, in comparison with 74.57 and 78.24% by pure MA and marketed MA, respectively. The anti-inflammatory efficacy of optimized SD was found to be significant as compared with pure and marketed MA ( < .05). The oral absorption of MA from optimized 20% SD was also noted as statistically significant as compared with pure MA ( < .05). The relative bioavailability of MA from 20 and 25% SDs was 2.97 and 2.24-folds higher than pure MA. The results of this study suggested that SDs prepared using hot-melt extrusion technology are capable to enhance palatability, anti-inflammatory efficacy, and oral bioavailability of MA in comparison with pure drug.
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http://dx.doi.org/10.1080/03639045.2019.1645161 | DOI Listing |
J Pharm Sci
January 2025
Department of Pharmaceutics, College of Pharmacy, University of Hail, Hail 81442, Saudi Arabia. Electronic address:
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View Article and Find Full Text PDFInt J Nanomedicine
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Department of Bio-Health Convergence, Kangwon National University, Chuncheon, 24341, Republic of Korea.
Purpose: Multi-walled carbon nanotubes (MWCNTs) were used as carriers for silver nanoparticles (AgNPs). In this process, MWCNTs were coated with mesoporous silica (MWCNT-Silica) for uniform and regular loading of AgNPs on the MWCNTs. In addition, astaxanthin (AST) extract was used as a reducing agent for silver ions to enhance the antioxidant, antibiofilm, and anticancer activities of AgNPs.
View Article and Find Full Text PDFColloids Surf B Biointerfaces
January 2025
Department of Biomaterials and Tissue Engineering, School of Advanced Technologies in Medicine, Isfahan University of Medical Sciences, Isfahan, Iran; Biosensor Research Center, Isfahan University of Medical Sciences, Isfahan, Iran.
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View Article and Find Full Text PDFAAPS PharmSciTech
January 2025
Molecular Pharmaceutics and Drug Delivery, College of Pharmacy, The University of Texas at Austin, Austin, Texas, USA.
Poly(lactide-co-glycolide) (PLGA) is widely used in a variety of long-acting injectables. However, its biodegradable nature creates potential chemical stability challenges during melt extrusion, where PLGA is exposed to elevated temperature (100-140 °C) for several minutes. This study evaluated the thermal stability of three PLGA grades (Resomer® 502, 502H, and 505) with varying molecular weights and chain-ends using a differential scanning calorimeter and twin-screw extruder.
View Article and Find Full Text PDFPharmaceutics
December 2024
Department of Pharmaceutics and Drug Delivery, School of Pharmacy, The University of Mississippi, Oxford, MS 38677, USA.
This study evaluates the efficacy of twin screw melt granulation (TSMG), and hot-melt extrusion (HME) techniques in enhancing the solubility and dissolution of simvastatin (SIM), a poorly water-soluble drug with low bioavailability. Additionally, the study explores the impact of binary polymer blends on the drug's miscibility, solubility, and in vitro release profile. SIM was processed with various polymeric combinations at a 30% / drug load, and a 1:1 ratio of binary polymer blends, including Soluplus (SOP), Kollidon K12 (K12), Kollidon VA64 (KVA), and Kollicoat IR (KIR).
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