title: Enhanced oral bioavailability of the antiretroviral efavirenz encapsulated in poly(epsilon-caprolactone) nanoparticles by a spray-drying method.
abstract: OBJECTIVE
  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.
  
  
  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.
  
  
  CONCLUSIONS
  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.
authors.affiliation: Polymers & Composites, Council for Scientific & Industrial Research Materials Science & Manufacturing, Council for Scientific & Industrial Research, Pretoria, South Africa.
authors.forename: Lesego
authors.initials: L
authors.lastname: Tshweu
authors.forename: Lebogang
authors.initials: L
authors.lastname: Katata
authors.forename: Lonji
authors.initials: L
authors.lastname: Kalombo
authors.forename: Diego A
authors.initials: DA
authors.lastname: Chiappetta
authors.forename: Christian
authors.initials: C
authors.lastname: Hocht
authors.forename: Alejandro
authors.initials: A
authors.lastname: Sosnik
authors.forename: Hulda
authors.initials: H
authors.lastname: Swai
mesh_terms: D000284:Administration, Oral; D000480:Alkynes; D000818:Animals; D019380:Anti-HIV Agents / Q000008:administration & dosage* / Q000493:pharmacokinetics*; D048588:Benzoxazines / Q000008:administration & dosage* / Q000493:pharmacokinetics*; D001682:Biological Availability; D002626:Chemistry, Pharmaceutical; D003521:Cyclopropanes; D008297:Male; D008855:Microscopy, Electron, Scanning; D053769:Nanocapsules / Q000008:administration & dosage / Q000737:chemistry / Q000648:ultrastructure; D050997:Nanomedicine; D036103:Nanotechnology; D010316:Particle Size; D011091:Polyesters / Q000737:chemistry; D051381:Rats; D017208:Rats, Wistar; D018894:Reverse Transcriptase Inhibitors / Q000008:administration & dosage / Q000493:pharmacokinetics; D017550:Spectroscopy, Fourier Transform Infrared; D014961:X-Ray Diffraction
chemical_list: D000480:Alkynes; D019380:Anti-HIV Agents; D048588:Benzoxazines; D003521:Cyclopropanes; D053769:Nanocapsules; D011091:Polyesters; D018894:Reverse Transcriptase Inhibitors; C016240:polycaprolactone; C098320:efavirenz
keywords: HIV; efavirenz; in vitro drug release; oral bioavailability enhancement; poly(epsilon-caprolactone) nanoparticle; spray drying