Biopharmaceutic study of an HIV-1 inhibitor peptide using nanosystems

Abstract

Women in Africa are disproportionately affected by human immunodeficiency virus type 1 (HIV-1) and many are unable or unwilling to negotiate condom use due to cultural/traditional behaviour or simply wants to conceive. For that reason, the development of a drug delivery system loaded with vaginal microbicide would be of greater benefit to inhibit the spread of HIV-1 not only in disadvantaged areas, like Africa, but also at global scale. In this study, different formulations containing a fusion inhibitor peptide as a microbicide have been prepared. These two preparations consist of two nanosystems, poly(lactic-co-glycolid acid (PLGA) coated with polyvinyl alcohol (PVA) nanoparticles (NPs) and 1-Palmitoyl-2-oleoyl-sn-glycero-3-phosphocholine (POPC) large unillamelar vesicles (LUVs), that improve tissue absorption, penetration and targeting for peptide anti-HIV-1 activity. PLGA-PVA NPs were formulated via solvent displacement and POPC LUVs via the hydration of thin film method, both formulations loaded with the peptide. Size, polidispersion index (PdI), zeta potential (Zpot) and entrapment efficiency (EE) were determined to evaluate their properties. It was necessary to evaluate the stability of the liposomes and nanoparticles at 4 ° C by measuring their size and polydispersity over a period of one month and a half. Both formulations were characterized to determine peptide release rate using a synthetic membrane (in vitro study) and vaginal mucosa permeation (ex vivo study). Previously studies had assayed the stability of the peptide using the same conditions