局部用辣椒碱传递体的制备及体外评价

目的:制备辣椒碱传递体,并对其质量进行评价。方法:采用高剪切分散乳化均质机制备辣椒碱传递体,并对其大小与结构、包封率、释放度及体外皮肤渗透性进行评价。结果:辣椒碱传递体结构为小单室,平均粒径150.6 nm,当脂质含量为8%时,包封率为96.7%。体外累积释放量随接受液中乙醇含量的提高而增加,不同基质大鼠腹部皮肤体外辣椒碱累积透皮量为:传递体>霜剂、混悬液。不同种类皮肤辣椒碱累积透皮量为:小鼠大鼠人,人体皮肤辣椒碱累积透皮量为:表皮膜真皮层、完整皮肤。结论:辣椒碱传递体包封率达到药典的规定(>80%),辣椒碱传递体的确可以增加辣椒碱的皮肤透过性,皮肤种类及皮肤的不同层次影响辣椒碱传递体的皮肤透过性。

Preparation and in vitro evaluations of topically applied capsaicin transfersomes

Objective: Capsaicin transfersomes were prepared and its quality specifications were evaluated.Method: Capsaicin transfersomes were prepared by high shear dispersing machine and evaluated on the entrapment efficiency,drugs release rate and in vitro skin permeation. Result: Capsaicin transfersomes is composed of single unilamellar vesicles,with average size of 150.6 nm.Capsaicin entrapment efficiency achieved 96.7% while concentration of lecithin used was 8%.cumulative release amount of capsaicin was in direct proportion to the ethanol concentration in the medium. The in vitro rate cumulative penetration rate of capsaicin was higher in transfersomes than in cream and suspension in rats.Adomen skin cumulative penetration rate in vitro of capsaicin transfersomes in mouse was significantly higher than that from rat and men.In the same way,cumulative penetration rate in vitro of capsaicin transfersomes through abdomen skin epidermal membrance was significantly higher than that with derma and full skin in men.Conclusion: Entrapment efficiency of capsaicin transfersomes reached 96.7%,meeting the criterion of China pharmacopia(>80%),skin penetration of capsaicin was enhanced by a capsaicin transfersomes preparation and was affected by diverse characters and levels of skin.