Promoting effect of positive polarity electret combined with azone on transdermal penetration of cyclosporin A / 第二军医大学学报

ABSTRACT

Objective To study the effects of positive polarity electret combined with different concentrations of azone in promoting the transdermal delivery of cyclosporin A, so as to explore the feasibility and the rule of electret combined with chemical enhancers in promoting transdermal delivery. Methods Cyclosporin A was used as the model drug in the present study. Positive polarity electret was prepared using corona charge technique. Franz diffusion cell system and HPLC techniques were applied to investigate the roles of positive polar electret, azone of different concentrations and their combination in promoting penetration of cyclosporin A in vitro. Results Satisfactory penetration promoting effects for cyclosporin A was observed in excised skin 24 h after exposure to +500 V, +1 000 V and +2 000 V electret. Compared to the control group, 1%, 3%, and 5% azone promoted the steady-state penetration rates of cyclosporin A by 6. 72, 2. 11, and 1. 43 folds after 24 h exposure. Combination of +1 000V electret plus 1% azone showed better penetration promoting effect than other combinations, but electret with different positive charges and different concentrations of azone showed no synergistic effect in promoting cyclosporin A penetration. Conclusion Positive polarity electret has a penetration promoting effect for transdermal delivery of cyclosporin A. Positive polarity electret and azone show no synergistic effect on promoting penetration of cyclosporin A.