Lipid Architectonics for Superior Oral Bioavailability of Nelfinavir Mesylate: Comparative in vitro and in vivo Assessment

Abstract

Nelfinavir mesylate (NFV), a human immunodeficiency virus (HIV) protease inhibitor, is an integral component of highly active anti retro viral therapy (HAART) for management of AIDS. NFV possesses pH-dependent solubility and has low and variable bioavailability hampering its use in therapeutics. Lipid-based particulates have shown to improve solubility of poorly water soluble drugs and oral absorption, thereby aiding in improved bioavailability. The current study compares potential of vesicular and solid lipid nanocarriers of NFV with drug nanocrystallites and microvesicular systems like cochleates in improving bioavailability of NFV. The paper outlines investigation of systems using in vitro models like in vitro lipolysis, in vitro release, and permeation through cell lines to predict the in vivo potential of nanocarriers. Finally, in vivo pharmacokinetic study is reported which provided proof of concept in sync with results from in vitro studies. Graphical Abstract ᅟ.

Spironolactone-Loaded LeciPlexes as Potential Topical Delivery Systems for Female Acne: In Vitro Appraisal and Ex Vivo Skin Permeability Studies

“…Further, the small particle size of the LeciPlexes is another important factor that contributes to their enhanced skin permeation. Other LeciPlex formulations have shown enhanced drug permeation through biological membranes [27,31,67].…”

Liposomes: Advancements and innovation in the manufacturing process

“…7) in the nano range with excellent shelf stability [85]. The system has successfully been explored for encapsulating various drugs like azelaic acid [86], carvedilol [87], idebenone [86], nelfinavir mesylate [88], quercetin [89,90], silibinin [91], and spironolactone [92]. Authors have also explored various biocompatible solvents such as transcutol, ethanol, glycofurol [93].…”

Antioxidant and Anti-Inflammatory Properties of Cherry Extract: Nanosystems-Based Strategies to Improve Endothelial Function and Intestinal Absorption

“…Otero et al [132] demonstrated that non-encapsulated bacteriophages were able to cross the intestinal barrier with respect to the encapsulated ones, which was probably because liposomes containing bacteriophages had a prolonged residence time in the stomach, thus adhering to the intestinal wall and protecting phages until they release. In another study, Belubbi et al [133] encapsulated nelfinavir mesylate (NFV) in liposomes and studied their permeability using the triple cell co-culture method. They found that the liposomes had a high NFV encapsulation efficiency, but no liposomes permeation was observed.…”