Co-encapsulation of efavirenz and curcumin within polymeric nanomicelles: preliminary studies

FUENTES P.; RIEDEL J.; GARCES M.; MORETTON M.A.; HOCHT C.; EVELSON P.; BERNABEU E.; CHIAPPETTA D.A.

Congreso; 6ta Reunión Internacional de Ciencias Farmacéuticas (RICiFa 2020+1); 2021

In 2020 UNAIDS/WHO estimated that 37.7 million people were HIV positive. Recent studies haveshown that patients who are HIV positive and fall ill with COVID-19, have double the risk of mortalitythan those who are HIV negative. Efavirenz (EFV) is a first line antiretroviral drug with low oralbioavailability (40-45%) and low aqueous solubility (4 μg/mL). As of late, Curcumin (CUR) (a naturalcompound) has been become relevant as a potential anti-HIV drug. However, the development offormulations with CUR, are limited by its low aqueous solubility (0.6 μg/mL). Considering theselimitations, nanomicelles of Soluplus® were developed to encapsulate EFV and CUR. Micellar sizewas determined by DLS and antioxidant activity of the micelles was measured by DPPH method. The water solubility of EFV and CUR increased 2500 and 3333 times, respectively. These nanomicelles present a size of ~100nm. Furthermore, when diluted (1/100) in different simulated biological fluids the nanosystems remained stable, even after 24 hours at 37 °C. The antioxidant properties of CUR were not affected by encapsulation. In addition, the in vitro cytotoxicity of the EFV and CUR nanomicelles; tested on macrophages (RAW 264.7), and the in vitro hemolysis study (< 2 %) demonstrated that the formulation presents an excellent safety profile.