Fang Jia-You, Sung K C, Wang Jhi-Joung, Chu Chin-Chen, Chen Kuan-Ting
Pharmaceutics Laboratory, Graduate Institute of Natural Products, Chang Gung University, Kwei-Shan, Tao-Yuan, Taiwan.
J Pharm Pharmacol. 2002 Oct;54(10):1329-37. doi: 10.1211/002235702760345392.
The in-vitro permeation of buprenorphine across skin was investigated to assess the effects of iontophoresis and electroporation on drug permeation from solutions as well as from hydrogels. Iontophoresis (0.3 mA cm(-2)) increased the buprenorphine permeation from solution by a factor of 14.27 as compared with passive diffusion; the application of electroporation increased the buprenorphine permeation from solutions by a factor of 8.45. The permeation experiments using cellulose membrane and stratum corneum (SC)-stripped skin as permeation barriers suggested that the enhancement with iontophoresis was primarily due to strong electrophoretic drift of buprenorphine molecules, whereas the enhancement seen with electroporation was mainly attributed to the creation of transient aqueous pores in the SC layer. Application of high-voltage pulses followed by iontophoresis resulted in a shorter permeation onset time from both solutions and hydrogels as compared with iontophoresis or electroporation alone. The charge repulsion between buprenorphine and chitosan vehicles as well as the competition effects of counter-ions for carboxymethylcellulose (CMC)-based polymers may account for the different permeation rates under electrical field. This study demonstrates the feasibility of using hydrogels for delivery of buprenorphine under the application of iontophoresis or electroporation, separately or together.
研究了丁丙诺啡经皮的体外渗透情况，以评估离子导入和电穿孔对药物从溶液以及水凝胶中渗透的影响。与被动扩散相比，离子导入（0.3 mA cm(-2)）使丁丙诺啡从溶液中的渗透增加了14.27倍；电穿孔的应用使丁丙诺啡从溶液中的渗透增加了8.45倍。使用纤维素膜和去除角质层（SC）的皮肤作为渗透屏障的渗透实验表明，离子导入的增强主要归因于丁丙诺啡分子强烈的电泳漂移，而电穿孔所见的增强主要归因于在SC层中形成瞬时水孔。与单独进行离子导入或电穿孔相比，施加高压脉冲后再进行离子导入可使溶液和水凝胶的渗透起始时间更短。丁丙诺啡与壳聚糖载体之间的电荷排斥以及抗衡离子对羧甲基纤维素（CMC）基聚合物的竞争效应可能解释了电场下不同的渗透速率。本研究证明了单独或联合使用离子导入或电穿孔时，使用水凝胶递送丁丙诺啡的可行性。
