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Solid Self-Microemulsifying Drug Delivery System for Improved Oral Bioavailability of Relugolix: Preparation and Evaluation.
Int J Nanomedicine
January 2025
School of Pharmacy, Jiangxi Medical College, Nanchang University, Nanchang, 330006, People's Republic of China.
Purpose: To improve the oral absorption of relugolix (RLGL), which has low oral bioavailability due to its low solubility and being a substrate of P-glycoprotein (P-gp). A solid self-microemulsifying drug delivery system of relugolix (RLGL-S-SMEDDS) was prepared and evaluated in vitro and in vivo.
Methods: The composition of the solid self-microemulsifying drug delivery system (S-SMEDDS) was selected by solubility study and pseudo-ternary phase diagram, and further optimized by Design-Expert optimization design.
Study of antiplasmodial activity, toxicity, pharmacokinetic profiles of n-methyl-isatin (CHISACN) derivative.
Exp Parasitol
January 2025
Post-graduate Program in Studies in Natural Products and Synthetic Bioactive, Federal University of Paraíba, João Pessoa, PB, Brazil; Laboratory of Toxicological Tests, Federal University of Paraíba, João Pessoa, PB, Brazil; Post-graduate Program in Studies in Development and Technological Innovation in Medicines, Federal University of Paraíba, João Pessoa, PB, Brazil.
One of the main factors that have made it difficult to control malaria is the large number of parasites that are resistant to the usual antimalarial drugs. Therefore, the development of new drugs that are more effective and with low toxicity for humans is necessary. In this work, we evaluated the adduct 2-(3-hydroxy-1-methyl-2-oxoindolin-3-yl) acrylonitrile, also called CHISACN, as a potential antimalarial through in vitro studies, and evaluated its effects in silico and in vivo toxicology.
View Article and Find Full Text PDFUnlabelled: Early phase dose-finding (EPDF) trials are key in the development of novel therapies, with their findings directly informing subsequent clinical development phases and providing valuable insights for reverse translation. Comprehensive and transparent reporting of these studies is critical for their accurate and critical interpretation, which may improve and expedite therapeutic development. However, quality of reporting of design characteristics and results from EPDF trials is often variable and incomplete.
View Article and Find Full Text PDFProteins and DNA Sequences Interacting with Tanshinones and Tanshinone Derivatives.
Int J Mol Sci
January 2025
Department of Pharmacology and Therapeutics, School of Biomedical Sciences, College of Health Sciences, Makerere University, Kampala P.O. Box 7062, Uganda.
Tanshinones, biologically active diterpene compounds derived from , interact with specific proteins and DNA sequences, influencing signaling pathways in animals and humans. This study highlights tanshinone-protein interactions observed at concentrations achievable in vivo, ensuring greater physiological relevance compared to in vitro studies that often employ supraphysiological ligand levels. Experimental data suggest that while tanshinones interact with multiple proteomic targets, only a few enzymes are significantly affected at biologically relevant concentrations.
View Article and Find Full Text PDFThe Rise of Fentanyl: Molecular Aspects and Forensic Investigations.
Int J Mol Sci
January 2025
Legal Medicine, Department of Medical, Surgical and Advanced Technologies "G.F. Ingrassia", University of Catania, 95123 Catania, Italy.
Fentanyl is a synthetic opioid widely used for its potent analgesic effects in chronic pain management and intraoperative anesthesia. However, its high potency, low cost, and accessibility have also made it a significant drug of abuse, contributing to the global opioid epidemic. This review aims to provide an in-depth analysis of fentanyl's medical applications, pharmacokinetics, metabolism, and pharmacogenetics while examining its adverse effects and forensic implications.
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