胰岛素通过电致孔的经皮传输特性

Transdermal transport characteristics of insulin measured using electroporation

为强化胰岛素在电致孔下的经皮渗透,采用在胰岛素溶液中添加表面活性剂十六烷基三甲基溴化铵(CTAB)的方法,得到了不同聚集程度的胰岛素,研究了胰岛素的聚集程度及供给液的pH值对胰岛素在电致孔下的传质通量和经皮渗透效率的影响。结果表明,胰岛素分子的聚集和其在皮肤中的滞留,是限制胰岛素经皮渗透量提高的主要因素。单体胰岛素分子在脉冲的时间常数为6～8ms时,经皮渗透通量较聚合度接近6的胰岛素提高了3～5倍,且将近70%的胰岛素透过了皮肤。当溶液的pH在4.0～5.0时,胰岛素的经皮渗透通量相对较高。

This paper reports an initial study to enhance transdermal insulin delivery. Insulin in various association states was prepared in the presence of cetyltrimethyl ammonium bromide (CTAB). The transdermal flux and efficiency of the insulin in varied association states through the local transport regions (LTRs) created during electroporation were investigated using in vitro experiments with mouse skin. The main problems encountered during transdermal insulin delivery via electroporation were self-association of the insulin molecules into aggregates and entrapment of the insulin in the epidermis. The transdermal flux of insulin with less aggregation in the presence of CTAB was improved 3～5 fold with over 70% of the total transported insulin detected in the receiver compartment under pulses with the duration of 6～8 ms. The transdermal transport of insulin was shown to be influenced by the pH of the donor solution with the highest transdermal insulin flux at pH of 4.0～5.0.