4.7 Article

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

期刊

NANOMEDICINE
卷 9, 期 12, 页码 1821-1833

出版社

FUTURE MEDICINE LTD
DOI: 10.2217/NNM.13.167

关键词

efavirenz; HIV; in vitro drug release; oral bioavailability enhancement; poly(epsilon-caprolactone) nanoparticle; spray drying

资金

  1. Ministry of Science, Technology and Productive Innovation (Argentina)
  2. National Research Foundation (South Africa)

向作者/读者索取更多资源

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.

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