| 摘要: |
| 目的探索盐酸青藤碱在微针阵列作用下的透皮给药规律与微针促进药物透皮吸收的机制。方法高效液相色谱法测定青藤碱的含量,裸鼠皮肤用微针阵列预刺处理,采用水平双室扩散池法研究微针的针尖形状、刺入力、滞留时间以及阵列数对于盐酸青藤碱透皮给药的影响规律。将微针预刺处理的皮肤制备成切片,并用显微镜观察皮肤的变化。结果微针阵列预刺处理与被动扩散比较能显著提高盐酸青藤碱透皮给药的累积渗透量(P<0.01),但平顶微针比尖顶微针更能有效促进药物的透皮吸收；药物的累积渗透量随着微针处理皮肤的刺入力的增加而增加,但当刺入力超过5 |
| 关键词: 盐酸青藤碱 微针阵列 皮肤投药 |
| DOI：10.3724/SP.J.1008.2011.0767 |
| 投稿时间：2011-03-26修订日期：2011-05-30 |
| 基金项目: |
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| Studies on transdermal delivery of sinomenine hydrochloride through mouse skin treated by microneedle arrays |
| LI Wei-ze1*,YAN Jing-hua2,ZHAO Ning1,LIU Shao-jing1 |
| (1. Department of Pharmaceutics, Xi’an Medical University, Xi’an 710021, Shaanxi, China;2. Department of Traditional Chinese Herbs, School of Life Science, Northwest University, Xi’an 710069, Shaanxi, China) |
| Abstract: |
| Abstract: Objective To study the characteristics and mechanism of solid silicon microneedle arrays deliver sinomenine hydrochloride (SH) transport across hairless rat skin. Methods The amount of SH was determined by HPLC system. Hairless rat skin pretreated with microneedle arrays by hand. The side-by-side diffusion cells were used to investigate the effects of needlepoint shape, different insertion force, retention time and number of microneedles on the SH transdermal drug delivery. Histological examination of skin samples after piercing by microneedles was conducted on paraffin sections and then viewed by brightfield microscopy. Results The skin pretreated with microneedle arrays resulted in a remarkable enhancement of SH transport compared with passive difussion, the flat tipped microneedles were better than sharp tipped microneedles for enhancing skin permeability. The permeated SH increased with the enhancement of insertion force; however, as the insertion force exceeded 5.0 N the permeated SH didn’t increase obviously any more. The skin permeability enhanced with the increase of retention time, as the retention time exceeded 1.0 min, the retention time would not significantly affect the transport ability of the skin. Although skin permeation increased as the microneedles number increased, yet there was no linear correlation between them. The micro-conduits created in skin by microneedles piercing were validated by histological examination. Conclusion The microneedles were able to pierce into skin and form conduits, the formed conduits in skin greatly increased the skin permeability of SH. These results showed that the microneedle arrays may be an efficient and promising technology for transdermal drug delivery of SH. |
| Key words: sinomenine hydrochloride microneedle arrays cutaneous administration |
