【作者】 陈华兵； 郑静南； 张俊勇； 赵英俊； 杨祥良；

【Author】 CHEN Hua-bing1, ZHENG Jing-nan1, ZHANG Jun-yong2, ZHAO Ying-jun2*, YANG Xiang-liang1* ( 1 Institute of Materia Medica, College of Life Science and Technology; 2 School of Mechanical Science and Engneering,Huazhong University of Science and Technology, Wuhan 430074,China)

【机构】 华中科技大学生命科学与技术学院药物研究所； 华中科技大学机械科学与工程学院；

【摘要】 目的不锈钢微针阵经皮给药的研究。考察离体大鼠皮肤经不同针形微针预处理相同时间、相同针形微针预处理不同时间后,模型药物鬼臼毒素经大鼠皮肤的透皮能力。方法微针预处理大鼠皮肤后,用改进的Franz扩散池研究鬼臼毒素对皮肤的透皮速率。高效液相色谱法测定鬼臼毒素的含量。结果皮肤经微针预处理后进行鬼臼毒素透皮,其透皮速率是未经微针处理皮肤的5～11倍。三角形微针、梯形微针、矛形微针对鬼臼毒素的促渗能力依次增强,此三种微针预处理皮肤后引起的鬼臼毒素透皮速率分别为2.63μg·cm-2·h-1,5.35μg·cm-2·h-1,10.10μg·cm-2·h-1。不同针形微针所引起的鬼臼毒素在皮肤中的滞留量有显著差异。采用同种针形微针预处理皮肤时间越长,鬼臼毒素的透皮速率越大,微针预处理皮肤1min,2min,3min所引起的药物透皮速率分别为3.29μg·cm-2·h-1,5.35μg·cm-2·h-1,11.82μg·cm-2·h-1。但微针预处理时间对皮肤中的药物滞留量无显著影响。结论微针用于药物经皮给药时,微针针形、微针的预处理时间对药物的经皮渗透具有重要影响。微针用于经皮给药时,微针针形和微针对皮肤的预处理时间是影响药物渗透的两个重要因素。不同针形微针在相同压力条件下预处理皮肤,在皮肤上所形成的微孔形态和尺寸不同,直接影响着药物的渗透。微针对皮肤预处理时间增加后有利于药物的经皮渗透。更多还原

【Abstract】 OBJECTIVE The purpose of this study was to investigate the in vitro transdermal delivery rates of podophyllotoxin with the pretreatment of miconeedles either of different needle-shapes pretreating mouse skin for the same time or the same needle-type pretreating skin for different time. METHODS The permeation flux of podophyllotoxin was determined in vitro using Franz diffusion cell fitted with the preteated mouse skin by microneedles.The content of podophyllotoxin was measured by HPLC. RESULTS The permeation rates of podophyllotoxin through the skin pretreated with microneedles are 5-11 times higher than that through the untreated one. The drug permeation rates enhanced by triangular microneedles, trapeziform microneedles, lanciform microneedles are increased from front to rear. And the corresponding permeation rates of podophyllotoxin are 2.63 μg·cm-2·h-1,5.35 μg·cm-2·h-1,10.10 μg·cm-2·h-1. The amount of drug left in pretreated mouse skin by microneedles of different needle-shapes are widely different. While using microneedles of the same needle-shape to pretreat skin for different time, the drug permeation rates grows higher as time prolongs, while the amounts of drug left in skin almost stay the same. Podophyllotoxin permeation rates are 3.29 μg·cm-2·h-1,5.35 μg·cm-2·h-1,11.82 μg·cm-2·h-1 corresponding to pretreating time lasting 1 min, 2 min, 3 min. CONCLUSION When used to enhance drug transdermal delivery, the needle-shape of microneedles and pretreating time on skin play quite important roles.更多还原