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  • Title: Enhanced oral bioavailability of the antiretroviral efavirenz encapsulated in poly(epsilon-caprolactone) nanoparticles by a spray-drying method.
    Author: Tshweu L, Katata L, Kalombo L, Chiappetta DA, Hocht C, Sosnik A, Swai H.
    Journal: Nanomedicine (Lond); 2014; 9(12):1821-33. PubMed ID: 24364871.
    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. Original submitted 2 May 2013; Revised submitted 4 September 2013.
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