Enhanced Oral Bioavailability of The Antiretroviral Efavirenz Encapsulated in Poly(Epsilon-Caprolactone) Nanoparticles by A Spray-Drying Method
2013; Future Medicine; Volume: 9; Issue: 12 Linguagem: Inglês
10.2217/nnm.13.167
ISSN1748-6963
AutoresLesego Tshweu, Lebogang Katata, Lonji Kalombo, Diego A. Chiappetta, Christián Höcht, Alejandro Sosnik, Hulda Swai,
Tópico(s)HIV/AIDS drug development and treatment
ResumoTo 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.EFV-loaded PCL NPs were produced by a double-emulsion/spray-drying method.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.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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