Anti HIV nanoemulsion formulation: optimization and in vitro-in vivo evaluation

Int J Pharm. 2014 Feb 28;462(1-2):129-34. doi: 10.1016/j.ijpharm.2013.12.038. Epub 2013 Dec 25.

Abstract

The objective of the present work is to develop a dose adjustable nanotechnology based liquid formulation of efavirenz with improved bioavailability for HIV therapy. Nanoemulsion of efavirenz was developed using phase inversion composition method with the help of ternary phase diagram. Globule size of the o/w nanoemulsion was studied with the help of dynamic light scattering and further confirmed with TEM analysis. Optimized formulations were subjected for in vitro dissolution studies and in vivo studies were done in rats to calculate pharmacokinetics parameters and compared with efavirenz suspension. TEM results revealed that the globule size of optimized formulation was less than 30 nm. In vitro release profile showed more than 80% release within 6 h which was highly significant (p>0.05) and pharmacokinetic studies also proved a promising in vivo absorption profile when compared to the efavirenz suspension. The developed nanoemulsion proved to be an effective dose adjustable formulation of efavirenz for pediatric HIV therapy.

Keywords: Condensation method; Efavirenz; Nanoemulsion; Phase inversion composition.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Alkynes
  • Animals
  • Benzoxazines / administration & dosage*
  • Benzoxazines / pharmacokinetics
  • Biological Availability
  • Chemistry, Pharmaceutical / methods
  • Cyclopropanes
  • Emulsions
  • Female
  • Light
  • Microscopy, Electron, Transmission
  • Nanoparticles*
  • Nanotechnology / methods*
  • Particle Size
  • Rats
  • Rats, Wistar
  • Reverse Transcriptase Inhibitors / administration & dosage*
  • Reverse Transcriptase Inhibitors / pharmacokinetics
  • Scattering, Radiation
  • Solubility

Substances

  • Alkynes
  • Benzoxazines
  • Cyclopropanes
  • Emulsions
  • Reverse Transcriptase Inhibitors
  • efavirenz