Development of ethosome containing bitter melon (Momordica charantia Linn.) fruit fraction and in Vitro skin penetration

Abstract

Objective: Bitter melon fruit, which is containing charantin, has poor penetration through the skin. This problem can be solved with the lipid vesicle called ethosomes that offers better skin penetration. This study was aimed to develop ethosomes for improving skin penetration ability of charantin. Methods: Bitter melon was extracted with ethanol 80% and fractionated with dichloromethane. Ethosomes were formulated with a various concentration equal to 2% (F1), 3% (F2) and 4% (F3) of bitter melon fruits fraction (BMFF) and prepared using thin layer hydration method. The obtained ethosomes were characterized, then the penetration study was conducted using Franz diffusion cells. Results: The results showed that the BMFF was a dry, brown-greenish fraction and gave a positive test for a steroid. The entrapment efficiency of ethosomes F1, F2 and F3 was 91.50 ± 0.40%, 92.62 ± 0.26% and 83.85 ± 1.10%, respectively. Moreover, the particle size (Dv90) of ethosomes F1, F2 and F3 was 1083.33 ± 15.27 nm, 1736.67 ± 11.55 nm and 1976.67 ± 5.77 nm, respectively. Ethosomes F1, F2 and F3 resulted polydispersity index of 0.42 ± 0.02, 0.35 ± 0.05 and 0.50 ± 0.11, as well as zeta potential of -54.33 ± 0.75, -57.50 ± 0.44 and -50.60 ± 0.98, respectively. Besides, all ethosomes had a spherical shape. The research revealed that ethosome F2 was the optimal ethosome among another formulas. Cumulative percentage of penetrated stigmasterol glycoside for ethosome F2 was 18.25 ± 0.08%, while the control solution did not penetrate within 20 h. Conclusion: This research demonstrated that the ethosome could increase the skin penetration of stigmasterol glycoside, which is charantin content, from the fraction of bitter melon fruit.