alexa Abstract | Solubility Enhancement of Poorly Water Soluble Drug Efavirenz by Solid Self Emulsifying Drug Delivery Systems


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Research Article Open Access

Abstract

Efavirenz is a non-nucleoside reverse transcriptase inhibitor (NNRTI) which has the poor aqueous solubility of 4-9 μg/ml.Currently a number of technologies are available to deal with the poor solubility, dissolution rate and bioavailability of insoluble drugs. One of the promising techniques is Self‐Micro Emulsifying Drug Delivery Systems (SMEDDS). Self emulsifying drug delivery system has gained more attention due to enhanced oral bio-availability enabling reduction in dose, more consistent temporal profiles of drug absorption, selective targeting of drug(s) toward specific absorption window in GIT. The main objective of this study is to improve the solubility of efavirenz by formulating in to a self-emulsifying drug delivery system with improved dissolution rate for the oral delivery of poorly water-soluble antiretroviral agent.. Solubility was determined in various oils, surfactants and co surfactants. Ternary phase diagrams were constructed to evaluate the micro emulsification region. Liquid SEDDS were prepared using LLWL 1349, Labrafac PG as oils and cremophor EL, cremophor RH40 as surfactants and labrasol, transcutol HP as co-surfactants. Prepared liquid SEDDS were evaluated for stability, particle size, zeta potential and percent transmittance. Selected liquid formulations were converted to solid SEDDS by adsorbing onto a solid carrier Neusilin. Prepared solid SEDDS were evaluated for flow properties and in-vitro drug release studies. Results proved that prepared solid SEDDS have good flow properties and improved drug solubility and dissolution profiles (99.95%) when compared to pure efavirenz.

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Author(s): M. Sunitha Reddy, N. Srikanth Reddy, S. Mallikarjun Reddy

Keywords

Adsorption, antiretroviral drug, dissolution rate, neusilin, solid- SEDDS, Liver Inflammation

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