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Nanocrystals (NCs), a colloidal dispersion system formulated with stabilizers, have attracted widespread interest due to their ability to effectively improve the oral bioavailability of poorly water-soluble drugs. The stabilizer plays a key role because it can affect the physical stability and even the oral bioavailability of NCs. However, how stabilizers affect the bioavailability of NCs remains unknown. In this study, F68, F127, HPMC, and PVP were each used as a stabilizer to formulate naringenin NCs. The NCs formulated with PVP exhibited excellent release behaviors, cellular uptake, permeability, oral bioavailability, and anti-inflammatory effects. The underlying mechanism is that PVP effectively inhibits the formation of naringenin dimer, which in turn improves the physical stability of the supersaturated solution generated when NC is dissolved. This finding provides insights into the effects of stabilizers on the performances of NCs and supplies valuable knowledge for the development of poorly water-soluble drugs.
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http://dx.doi.org/10.1016/j.ajps.2022.09.001 | DOI Listing |
J Sci Food Agric
September 2025
Graduate School of Environmental and Human Sciences, Meijo University, Nagoya, Japan.
Background: Astaxanthin Z-isomers have attracted much attention because recent studies have demonstrated that they exhibit greater bioavailability and biological activity than the naturally predominant all-E-isomer. However, the plasma appearance and tissue distribution of astaxanthin isomers when administered with a diet rich in astaxanthin Z-isomers are largely unknown. To understand the health benefits and safety of astaxanthin Z-isomers, it is important to study the in vivo kinetics of the isomers.
View Article and Find Full Text PDFEur J Pharm Sci
September 2025
Department of Medicinal Chemistry, Uppsala University, SE-75123 Uppsala, Sweden. Electronic address:
Subcutaneous (SC) injection is the primary alternative to oral administration for therapeutic proteins and peptides. However, bioavailability and absorption rate are often variable and difficult to predict. Therefore, there is a need for new biorelevant and predictive SC in vitro methods.
View Article and Find Full Text PDFInt J Biol Macromol
September 2025
Department of Pharmaceutics and Industrial Pharmacy, Faculty of Pharmacy, Badr University in Cairo (BUC), Badr City, Cairo, 11829, Egypt.
Famotidine (FMD) is an H₂-receptor antagonist with limited oral bioavailability and a short plasma half-life (2.5-4 h). Silk fibroin-chitosan nanoparticles (FBN-CS-NPs) represent a novel nanocarrier approach for treating peptic ulcers, combining biocompatibility, mucoadhesiveness, and pH-sensitive release.
View Article and Find Full Text PDFBioorg Chem
August 2025
College of Pharmacy and Graduate School of Pharmaceutical Sciences, Ewha Womans University, Seoul 03760, Republic of Korea. Electronic address:
Nucleoside analogs have served as the cornerstone of antiviral therapy by acting as antimetabolites that disrupt viral DNA or RNA synthesis, thereby effectively inhibiting viral replication. Despite their clinical success, many nucleoside-based antivirals suffer from intrinsic limitations such as poor lipophilicity, low membrane permeability, and rapid metabolic degradation, all of which compromise oral bioavailability and therapeutic efficacy. To address these challenges, lipid conjugation has emerged as a promising prodrug strategy that enhances pharmacokinetic properties, improves cellular uptake, and enables targeted delivery.
View Article and Find Full Text PDFDrug Metab Dispos
August 2025
Department of Pharmaceutical Sciences, College of Pharmacy and Pharmaceutical Sciences, Washington State University, Spokane, Washington; Division of Translational and Clinical Pharmacology, Cincinnati Children's Hospital Medical Center, Cincinnati, Ohio. Electronic address:
Hypogonadism, characterized by low testosterone blood levels, affects 3%-5% of males worldwide. Oral testosterone undecanoate (TU) is emerging as a key route of administration due to its better ease of administration; however, it suffers from variable pharmacokinetics and pharmacodynamics. The variability is majorly attributed to intestinal glucuronidation of testosterone to its hydrophilic metabolite, testosterone glucuronide (TG), formed by the polymorphic uridine 5'-diphospho-glucuronosyltransferase 2B17 (UGT2B17).
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