Long Xiao-ying, Luo Jia-bo, Li Li-ren, Lin Dan, Rong Hui-si, Huang Wei-min
Southern Medical University, Guangzhou 510515, China.
Zhongguo Zhong Yao Za Zhi. 2006 Jun;31(12):981-4.
Capsaicin transfersomes were prepared and its quality specifications were evaluated.
Capsaicin transfersomes were prepared by high shear dispersing machine and evaluated on the entrapment efficiency, drugs release rate and in vitro skin permeation.
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.
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.
制备辣椒素传递体并评价其质量规格。
采用高剪切分散机制备辣椒素传递体，并对其包封率、药物释放速率和体外皮肤渗透进行评价。
辣椒素传递体由单室脂质体组成，平均粒径为150.6nm。当卵磷脂用量为8%时，辣椒素包封率达到96.7%。辣椒素的累积释放量与介质中的乙醇浓度成正比。在大鼠中，辣椒素传递体的体外累积渗透速率高于乳膏和混悬液。小鼠腹部皮肤辣椒素传递体的体外累积渗透速率显著高于大鼠和人体。同样，辣椒素传递体经人体腹部皮肤表皮膜的体外累积渗透速率显著高于真皮和全皮。
辣椒素传递体的包封率达到96.7%，符合中国药典标准（>80%），辣椒素传递体制剂可增强辣椒素的皮肤渗透性，且受皮肤不同性质和层次的影响。
