Fabrication and evaluation of self-nanoemulsifying oil formulations (SNEOFs) of Efavirenz

Abstract

The current work designed to fabricate and evaluate self-nanoemulsfying oil formulations (SNEOFs) of Efavirenz (Efz) a BCS class II drug with the objective of increasing its solubility as well as in vitro dissolution rate for improvisation of bioavailability. Preliminary screening of drug which includes solubility, emulsifying ability and ternary phase diagrams was carried out to fabricate SNEOFs. Various thermodynamic stability studies were exercised to find out the stable SNEOFs. Robustness to dilution, % transmittance and turbidity, droplet size analysis, TEM study, cloud point measurement, viscosity and refractive index were executed on the stable SNEOFs to characterize the delivery system. FTIR study was adopted for the compatibility of the additives with the drug. In vitro release profiles of SNEOFs compared with Efz, percent dissolution efficiency (DE) and dissolution half-life (t₅₀) were evaluated. A low percent DE (30.12%) and high t₅₀ was obtained for Efz whereas all SNEOFs showed a DE of greater than 78.48% and less than 9 min t₅₀. The optimized SNEOFs (F8) demonstrated a significant (p < 0.05) increase in bioavailability over Efz. Thus the designed optimized delivery system could be instrumental in increasing aqueous solubility of Efz, improving its release performance and enhancement of oral absorption.

Graphical Abstract

Keywords:

• Dissolution efficiency (DE)
• GPE810
• SNEOFs
• TEM
• Turbidity

Acknowledgements

The authors appreciatively acknowledge the Head, Sophisticated Analytical Instruments Facility STIC, Cochin University, Kerala, India for providing facilities for TEM analysis. The authors wish to thank Dr. S. B. Senapati, Department of Translational Research, Institute of Life Sciences (ILS), Bhubaneswar, India for his generous guidance in conduct of in vivo study. The authors are grateful to Dr. V. Badireenath Konkimalla, School of Biological Sciences, National Institute of Science Education and Research (NISER), Bhubaneswar, India for providing the necessary facility for particle size analysis. The authors are also thankful to Dr. Sanjay Kumar Swain, Central Instrumentation Facility, Birla Institute of Technology, Mesra, Ranchi, Jharkhand, India for his kind support for FTIR studies.