连翘不同活性成分柔性纳米脂质体透皮给药的研究  

Transdermal absorption of flexible nanoliposomes of different active ingredients of forsythia suspensa

作　　者：杨文婧[1] 程昊[1] 刘婷[1] 李伟泽[2] 郝保华[1] 

机构地区：[1]西北大学生命科学学院中药系,陕西西安710069 [2]中国药科大学药学院,江苏南京210009

出　　处：《中成药》2010年第4期577-581,共5页Chinese Traditional Patent Medicine

基　　金：西北大学研究生创新基金资助项目(08YJC23)

摘　　要：目的:制备连翘不同活性成分柔性纳米脂质体,并考察其透皮吸收规律。方法:采用薄膜分散法制备连翘苷以及连翘挥发油与连翘苷相结合的柔性纳米脂质体,并对其形态及粒径大小进行分析;用改良的Franz扩散池,以离体小鼠皮肤为透皮屏障,以连翘苷为指标,用HPLC法测定其在接收池中的含量,进行连翘不同活性成分柔性纳米脂质体与连翘苷水溶液的体外透皮实验;计算累积渗透量、透皮渗透速率并进行比较。结果:制备的连翘苷柔性纳米脂质体(WN组)的平均粒径为(180.7±13.69)nm,Zata电位为-48.8 mV,对连翘苷的平均包封率为(82.53±2.68)%;连翘挥发油与连翘苷相结合的柔性纳米脂质体(OWN组)的平均粒径为(212.3±15.31)nm,Zata电位为-51.2 mV,对连翘苷的平均包封率为(70.49±1.06)%。OWN组8 h累积渗透量为(291.92±23.22)μg/cm2,8 h透皮速率为36.49μg/(cm2.h),分别为连翘苷水溶液(WS组)和WN组的6.10和1.92倍,差异有统计学意义(P<0.01)。结论:柔性纳米脂质体显著加速了药物进入皮肤的能力,连翘挥发油的加入更是促进了这一过程。AIM： To prepare flexible nanoliposomes made from active ingredients,phillyrin and volatile oil,from forsythia suspense and study their transdermal delivery system.METHODS： Flexible nanolipsomes of phill-yrin（WN group） and phillyrin in combination with forsythia volatile oil（OWN group） were prepared by the meth-od of membrane-dispersion.Its appearance and particle sizes were measured.Transdermal experiments were carried out on the modified Franz diffusion pool through in vitro mouse skin.HPLC was applied to determining the phillyrin content to compare transdermal rate and cumulative permeation amount of various flexible nanoliposomes.RESULTS： The particle size of the WN group was（180.7 ± 13.69）nm,the Zata potential was-48.8 mV,the average encapsulation percentage was（82.53 ± 2.68）%;the particle size of the OWN group was（212.3 ± 15.31）nm,Zata potential was-51.2 mV,the average encapsulation percentage was（70.49 ± 1.06）%.The accu-mulated permeation amount of the OWN group in 8 hours was（291.92 ± 23.22） μg/cm2,its transdermal permea-bility in 8 hours was 36.49 μg/（cm2.h）,which was 6.10 folds that of the WS group and 1.92 folds that of the WN group.This difference had statistical significance（P 0.01）.CONCLUSION： Flexible nanoliposomes can significantly speed up the drug＇s permeation rate of entering the skin,and the addition of volatile oil of forsythia sus-pensa promote the transdermal delivery.

关 键 词：连翘 柔性纳米脂质体 透皮给药 

分 类 号：R944[医药卫生—药剂学]