earticle

영어

Megestrol acetate (MGA) is an appetite stimulant indicated for cachexia in patients with AIDS or cancer [1]. MGA is practically insoluble in water. The commercial formulation is available in microcrystal dispersion which shows extremely low oral absorption and large variation by food intake [2]. We designed new nano-formulation of megestrol acetate to enhance an oral bioavailability of megestrol acetate and studied the pharmacokinetic properties of our formulation under fed and fasting conditions.In this study, we designed nanoemulsions for the enhanced oral bioavailability of MGA. Oil, surfactant and cosurfactant were selected base on the solubility study. The mean particle size of nanoemulsions was estimated on zeta-sizer (ZS90, Malvern, England). Dissolution of MGA was estimated on dissolution tester (U.S. Pharmacopeia, Dissolution test, Apparatus 2). Relative oral bioavailability of our nano-formulation of MGA was compared with the commercial product (Megace® oral suspension, Bristol-Myers Squibb Co.) against dogs on fed and tasted state following cross-over design. The MGA nanoemulsions have 25nm of droplet size and over 80 % of dissolution rate. Relative oral bioavailability of MGA nanoemulsions compared to commercial oral suspension was 450 %, 150% in fasted and fed state, respectively.New nanoemulsions formulation of MGA was successfully designed and showed a good feasibility for the further clinical study. The enhanced oral bioavailability of MGA could assure the more reliable cancer chemotherapy in future.