Preparation and in vitro Transdermal Penetration of Capsaicin Liposomes / 中国药师

ABSTRACT

Objective:To prepare capsaicin liposomes and study the feasibility by in vitro percutaneous penetration test. Meth-ods:Capsaicin liposomes were prepared by a film-ultrasonic method. The best formula was screened by orthogonal test based on single factor studies with the entrapment efficiency as the index. The improved Franz diffusion cells were used to study the transdermal pene-tration of capsaicin suspensions, capsaicin liposomes and capsaicin ointments, and the cumulative penetration amount through the isola-ted rat skin was compared. Results:The optimal formula of capsaicin liposomes were as follows:the ratio of capsaicin to lipids was 1∶5;the amount of Tween-80 was 100 mg;the amount of vitamin E was 50 mg;10 ml dichloromethane was used as the solvent. The op-timal pH value of the external phase was 6. 5 with the volume of 10 ml. The ultrasonic time was 8 min. The order of 12-hour cumulative penetration amount was capsaicin liposomes>capsaicin-PBS suspensions>capsaicin ointments. Capsaicin liposomes had the highest 12-hour cumulative penetration amount and showed obvious sustained-release property. Conclusion:Capsaicin liposomes have high en-trapment efficiency, good percutaneous penetration and sustained-release property, and the preparation technology is simple.