Henry S, McAllister D V, Allen M G, Prausnitz M R
Institute for Bioengineering and Bioscience, School of Chemical Engineering, Georgia Institute of Technology, Atlanta, Georgia 30332, USA.
J Pharm Sci. 1998 Aug;87(8):922-5. doi: 10.1021/js980042+.
Although modern biotechnology has produced extremely sophisticated and potent drugs, many of these compounds cannot be effectively delivered using current drug delivery techniques (e.g., pills and injections). Transdermal delivery is an attractive alternative, but it is limited by the extremely low permeability of skin. Because the primary barrier to transport is located in the upper 10-15 micron of skin and nerves are found only in deeper tissue, we used a reactive ion etching microfabrication technique to make arrays of microneedles long enough to cross the permeability barrier but not so long that they stimulate nerves, thereby potentially causing no pain. These microneedle arrays could be easily inserted into skin without breaking and were shown to increase permeability of human skin in vitro to a model drug, calcein, by up to 4 orders of magnitude. Limited tests on human subjects indicated that microneedles were reported as painless. This paper describes the first published study on the use of microfabricated microneedles to enhance drug delivery across skin.
尽管现代生物技术已生产出极为精密和有效的药物，但使用当前的药物递送技术（如药丸和注射），许多此类化合物无法有效递送。透皮给药是一种有吸引力的替代方法，但它受到皮肤极低渗透性的限制。由于主要的转运屏障位于皮肤上部10 - 15微米处，而神经仅存在于更深层的组织中，我们使用反应离子蚀刻微加工技术制作微针阵列，其长度足以穿过渗透屏障，但又不至于长到刺激神经，从而潜在地不会引起疼痛。这些微针阵列可以轻松插入皮肤而不折断，并且在体外显示出可将人皮肤对模型药物钙黄绿素的渗透性提高多达4个数量级。对人体受试者的有限测试表明，微针被报告为无痛。本文描述了关于使用微加工微针增强药物经皮递送的首次发表研究。
