Enhanced oral bioavailability of the antiretroviral efavirenz encapsulated in poly(epsilon-caprolactone) nanoparticles by a spray-drying method.

Abstract

Aim: To encapsulate efavirenz (EFV) within poly(epsilon-caprolactone) (PCL) nanoparticles (NPs) and compare the oral pharmacokinetics with that of EFV-loaded micelles and pure EFV NPs. Materials & methods: EFV-loaded PCL NPs were produced by a double-emulsion/spray-drying method. Results: NPs displayed a hydrodynamic diameter of 200–250 nm. The encapsulation efficiency was 86–93% and the mass recovery was above 60%. X-ray diffraction indicated that drug and PCL underwent amorphization during the spray-drying process. Encapsulation within NPs significantly increased the maximum concentration in plasma and the bioavailability. Conclusion: EFV-loaded PCL NPs represent a promising platform to develop scalable pharmaceuticals with improved (bio)pharmaceutic performance.

Sustainable Development Goals

Research Article published by NANOMEDICINEVOL. 9, NO. 12

Keywords

HIV, Efavirenz, In vitro drug release, Oral bioavailability enhancement, Poly(epsilon-caprolactone) nanoparticle, Spray drying

Citation