Formulation and optimization of efavirenz nanosuspensions using the precipitation-ultrasonication technique for solubility enhancement

Abstract

Efavirenz is a non-nucleoside reverse transcriptase inhibitor, and is classified as BCS Class II API. Its erratic oral absorption and poor bioavailability make it a potential candidate for being formulated as a nanosuspension. The objective of this study was to formulate efavirenz nanosuspensions employing the antisolvent precipitation-ultrasonication method, and to enhance its solubility by reducing particle size to the nanometer range. The effects of different process parameters were studied and optimized with respect to particle size and poly dispersity index (PDI). The optimized formulation was also subjected to lyophilization, to further increase the solubility and stability, and the technology is potentially suited to a range of poorly water-soluble compounds.

Keywords::

• bioavailability
• drug delivery
• nanotechnology
• solubility enhancement
• solvent-antisolvent

Acknowledgements

The authors are thankful to M/s Emcure Pharmaceuticals Ltd. (India), for providing the gift sample of efavirenz. Author Sakshi Taneja acknowledges the All India Council for Technical Education, New Delhi for providing a JRF.

Declaration of interest

The authors report no conflicts of interest. The authors alone are responsible for the content and writing of the paper.