Department of Medicinal Chemistry, Elan Pharmaceuticals, 180 Oyster Point Boulevard, South San Francisco, CA 94080, United States.
Published: August 2010
AI Article Synopsis
Article Abstract
Herein we describe further evolution of hydroxyethylamine inhibitors of BACE-1 with enhanced permeability characteristics necessary for CNS penetration. Variation at the P2' position of the inhibitor with more polar substituents led to compounds 19 and 32, which retained the potency of more lipophilic analog 1 but with much higher observed passive permeability in MDCK cellular assay.
Ablative fractional laser-assisted drug delivery has gained attention as a promising method for enhancing dermal drug absorption and improving therapeutic outcomes in dermatological conditions, particularly for hypertrophic and keloid scars. However, despite the growing number of clinical trials and case reports supporting its efficacy, there remains a scarcity of robust evidence on the topical bioavailability and dermato-pharmacokinetics of drugs in human subjects. This study aimed to examine the enhancement of triamcinolone acetonide (TAC) bioavailability following treatment with a fractional Erbium-Doped Yttrium Aluminum Garnet (Er: YAG) laser.
Silicone contact lenses (SCL), as an emerging ocular drug delivery system, achieve controlled drug release. However, the existing drug loading methods have limitations such as low drug uptake, complicated operation process, poor welling rate and transmittance of the lens after drug loading. In this study, an effective microemulsion soaking method was proposed to increase the drug-loading capacity of silicone contact lenses.
The natural flavonoid Quercetin (QT) showed a potential for various health benefits, but its pharmaceutical applications are hindered by low solubility, permeability, and limited bioavailability. This research aimed to synthesize, develop and optimize polylactic acid co-glycolic acid (PLGA) nanobubbles using solvent evaporation method as a sustained delivery system for QT, thus improving stability and bioavailability. Through a four-factor, three-level Box Behnken Design, 29 experimental runs were carried out to optimize QT-PLGA nanobubbles.
Red grapes contain resveratrol (Resv), a polyphenol with anti-inflammatory, anti-diabetic, and anticancer properties. In this study, in silico molecular docking was used to assess the binding affinity of Resv to target proteins. Resv was encapsulated in PEGylated liposomes (LNPs) using Phospholipon 90G, cholesterol, and DSPE-mPEG.
Hypertension is a common disease; however, it is more prevalent in older adults, and its prevalence is increasing in younger populations. Numerous studies have revealed that hypertension and the composition and functionality of the intestinal flora are closely correlated. The balance of the intestinal flora, intestinal barrier integrity, and metabolite content of the intestinal flora play significant roles in the occurrence and progression of hypertension.
