Novel protease inhibitor-loaded Nanoparticle-in-Microparticle Delivery System for sustained release and improved bioavailability in the HIV therapy

IMPERIALE, JULIETA CELESTE; NEJAMKIN, PABLO; DEL SOLE, MARÍA JOSÉ; LANUSSE, CARLOS; SOSNIK, ALEJANDRO

Lisboa

Encuentro; 9th World Meeting on Pharmaceutics, Biopharmaceutics and Pharmaceutical Technology; 2014

Protease inhibitors (PIs) constitute a mainstay of the classic triad used to treat HIV. PIs exhibit low aqueous solubility that leads to a poor absorption with the resulting decrease in bioavailability and a rapid clearance. Both processes conduct to frequent administration schedules necessary to maintain stable plasma concentrations that usually leads to low patient compliance and treatment cessation. In this context, the design of a novel delivery system comprised of pure drug nanoparticles within mucoadhesive polymeric microparticles (NiMDS) represents a useful tool to improve bioavailability and control the payload release in order to reduce the frequency of administration. The main advantage of drug nanoparticles is its high superficial area that maximizes the drug loading and allows an improvement in the drug dissolution rate while the micro-structure by virtue of its muco-adhesive properties would permit to prolong the residence time of the drug at the absorption site, thus reaching higher bioavailability and lower administration frequency.