Design and Evaluation of Self-Nanoemulsifying Drug Delivery System of Flutamide

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%).

Development and Evaluation of Novel Self-Nanoemulsifying Drug Delivery Systems Based on a Homolipid from Capra hircus and Its Admixtures with Melon Oil for the Delivery of Indomethacin

“…In these cases, inclusion of carbosil increased the emulsification times beyond the 2 min time recommended for such systems [33]. Rapid self-emulsification occurs when the entropy change that favours dispersion of the SNEDDS is greater than the work required for increasing the surface area during dispersion [34]. Such free energy change should either be low, but positive, or negative [35].…”

Lipid Drug Carriers for Cancer Therapeutics: An Insight into Lymphatic Targeting, P-gp, CYP3A4 Modulation and Bioavailability Enhancement

“…The hydrophilic part of the micelles orients into the aqueous phase whereas hydrophobic chain forms the central part. [161][162][163] The overall solubilizing potential of the intestinal lumen is enhanced by the formation of mixed micellar phase, through lipid based formulations reducing precipitation of hydrophobic drugs. Their solubilizing potential is related with the ability to utilize enormous interfacial surface where the hydrophobic drug partitions.…”

Self-nanoemulsifying Drug Delivery System (Snedds) for Topical Delivery of Mangosteen Peels (Garcinia Mangostana L.,): Formulation Design and In vitro Studies

“…On the contrary, a decrease of electrostatic repulsive forces will cause phase separation. 29 In vitro test preparation used the principle of vertical type Franz Diffusion cell. Total percent of diffusion SNEDDS optimum formula for 8 hours was at 96,9223% and without SNEDDS was 18,9426 % It shows that the ethyl acetate fraction mangosteen peels formulation with SNEDDS can increase the penetration of α-mangostin pass through the stratum corneum.…”