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Enhanced Oral Bioavailability Of The Antiretroviral Efavirenz Encapsulated In Poly(epsilon-caprolactone) Nanoparticles By A Spray-drying Method.

Lesego L. Tshweu, L. Katata, L. Kalombo, D. Chiappetta, C. Hõcht, A. Sosnik, H. Swai
Published 2014 · Materials Science, Medicine

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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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