原花青素柔性纳米脂质体小鼠皮肤局部药代动力学研究.docVIP

PAGE PAGE 7 原花青素柔性纳米脂质体小鼠皮肤局部药代动力学研究 陈燕军1，张军斌2，熊欣1，武惠斌2，顼佳音1，金日显1，郁宝剑1，熊维政2，黄璐琦1* (l.中国中医科学院中药研究所，北京100700； 2.河南羚锐制药股份有限公司，河南 新县465550) [摘要] 目的：制备原花青素柔性纳米脂质体，考察原花青素在小鼠腹部皮肤的滞留量与时间的关系，及其局部经皮给药的药动学，探讨柔性纳米脂质体促进药物的经皮吸收的作用。方法：采用薄膜分散法制备原花青素柔性纳米脂质体，采用紫外-可见分光光度法测定不同时间给药皮肤中原花青素生物滞留量，采用DAS软件拟合药物动力学参数。结果：原花青素柔性纳米脂质体在小鼠皮肤中滞留量的动力学过程符合二室模型。结论：原花青素柔性纳米脂质体中有效成分能较快渗透进入皮肤，并在皮肤局部较长时间蓄积。 [关键词] 原花青素；柔性纳米脂质体；皮肤局部药代动力学 Dermatopharmacokinetic Studies of Proanthocyanidins Flexible Nanoliposomes in rat topical skin CHEN Yan-jun1, WU Hui-bin2, XIONG Xin1, SHI Lei2, XU Jia-yin, JIN Ri-xian1, YU Bao-jian1, XIONG Wei-zheng2, HUANG Lu-qi1* (1 Institute of Chinese Materia Medica , China Academy of Chinese Medical Science , Beijing 100700 , China ; 2 Henan LingruiPharmaceutical Company Ltd. Xinxian 465550) [Abstract] Objective: To prepare flexible nanoliposomes with Proanthocyanidins. To study the relationship between deposition and time of Proanthocyanidins in rats’ abdominal skin and it’s topical pharmacokinetics. To investigate the function of flexible nanoliposomes in enhancing the transdermal absorption of the encapsulated drug. Methods: To prepare flexible nanoliposomes with Proanthocyanidins using a film dispersion method, determine the relationship between deposition and time of Proanthocyanidins in rats’ abdominal skin by ultraviolet spectrophotometry, fit the pharmacokinetic parameters by DAS. Results: Depositions of different time in rats’ abdominal skin can be fitted with the two compartment model. Conclusion: The active ingredients of Proanthocyanidins flexible nanoliposomes can permeate through the skin effectively and lined long time. [Key words] Proanthocyanidins; Flexible Nanoliposomes; Dermatopharmacokinetic Studies of topical skin 柔性纳米脂质体（Flexible nanoliposomes），又称传递体、变形脂质体，是通过自身膜的高度变形性，以渗透压差为驱动力，能高效地穿透比它本身小数倍孔道的类脂聚集体。粒径多为数十至数百纳米，具有高 [收稿日期015） [基金项目] 中国博士后科学基金(20080430532) [第一作者] 陈燕军，博士，副研究员，研究方向：中药新型给药系统的研究，Tel：（010E-mail：ivycyj@163.com [通迅作者] *黄璐琦，博士，研