Efavirenz-loaded poly(epsilon-caprolactone)/poly(methacrylate) blend nanoparticles for sustained release in HIV

SEREMETA, KP; CHIAPPETTA, DA; SOSNIK, A

Natal

Congreso; 7th Latin American Congress of Artificial Organs and Biomaterials; 2012

Sociedad Latinoamericana de Biomateriales, Órganos Artificiales e Ingeniería de Tejidos (SLABO)

According to the latest World Health Organization fact sheets, approximately 40 million people are chronically infected with the HIV worldwide. A successful antiretroviral therapy is associated with a dramatic decrease in the Acquired Immunodeficiency Syndrome (AIDS)-associated mortality. The present work explored the development of poly(epsilon-caprolactone)/polymethacrylate blend nanoparticles (NPs) loaded with high payloads of the first-choice antiretroviral efavirenz as an approach to fine tune the release kinetics. NPs displaying hydrodynamic diameter between 90-550 nm were obtained by emulsion/solvent evaporation and nanoprecipitation methods. The encapsulation efficiency were greater than 90% and the drug weight content above 9%. The highly-positive surface (> +30 mV) rendered the nanosuspensions physically stable. The release profile from the different systems showed a first-order kinetics. However, NPs incorporating poly(methacrylate) showed a significantly slower release rate than pure poly(epsilon-caprolactone) ones. The developed NPs are a useful platform to investigate the targeting of antiretrovirals to the brain.