Abstract
Flutamide (FLT) is an antiandrogen drug for the treatment of prostate cancer. It has the drawback of poor water solubility and needs enhancement of its dissolution rate in simulated gastric fluids. Hence, it is prepared as self-nanoemulsifying drug delivery systems (SNEDDS) with an aim to enhance its dissolution rate. The objectives of the study are to develop SNEDDS of FLT and to characterize for particle size, self-nanoemulsification, and dissolution enhancement. Solubility of FLT was determined in various oils, surfactants, and cosurfactants. Sesame oil was selected as an oil phase, Tween 20 as surfactant, and PEG400 as cosurfactant due to their higher solubilization effect. Various formulations were prepared by simple mixing followed by vortexing. From studies, the optimized SNEDDS formulation was composed of FLT (8.04% w/w), sesame oil (24.12% w/w), Tween 20 (53.38% w/w), and PEG400 (14.46% w/w). The selected SNEDDS could be self-emulsified without precipitation upon simple mixing. The mean particle size of the SNEDDS was 148.7 nm and percent drug content was 99.66. The dissolution rate of FLT from SNEDDS was faster and higher in three different dissolution media such as 2% sodium lauryl sulfate (97.85%), simulated gastric fluid (0.1 N HCl containing 0.5% Tween 20) (95.71%), and simulated intestinal fluid (pH 6.8 buffer) (96.21%).
Highlights
The advent of combinatorial chemistry and highthroughput screening has resulted in the rapid identification of many highly potent new chemical entities
For the preparation of selfnanoemulsifying drug delivery systems (SNEDDS), sesame oil, Tween 20, and PEG 400 were chosen as an oil, surfactant, and cosurfactant
An optimized SNEDDS formulation of FLT consisting of FLT (8.04% w/w), sesame oil (24.12% w/w), Tween 20 (53.38% w/w), and PEG 400 (14.46% w/w) was successfully developed with an increased solubility and dissolution rate
Summary
The advent of combinatorial chemistry and highthroughput screening has resulted in the rapid identification of many highly potent new chemical entities. While these attributes conspire to provide optimized drug-receptor binding characteristics, they tend to result in poor drug solubility and poor membrane permeability characteristics. As solubility and permeability are considered prerequisites to oral absorption, many of these drugs exhibit poor and variable bioavailability.[1] Such drugs may be recognized by a highdose-to-solubility ratio, and bioavailability is frequently increased by coadministration of food.[2,3].
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