分层可溶性利多卡因聚合物微针的制备与穿刺效果研究

Preparation and Puncturing Effect of Lidocaine-Containing Polymer Microneedles with Stratified Solubility

为研究高效利多卡因分层可溶性微针的制备工艺和皮肤穿刺效果,利用聚二甲基硅氧烷(PDMS)微针模具,选用聚乙烯醇(PVA)、透明质酸钠(HA)和聚乙烯吡咯烷酮(PVP)为复合材料,探究分步浇铸法和浇注黏合法制备微针阵列。同时,利用显微镜观察微针形态并且测量微针的形态,选用小鼠腹部皮肤进行穿刺试验并进行冷冻切片表征微针穿刺效果。结果表明,利多卡因分层可溶性微针成型率达100%且成型周期缩短至4 h以内,药物主要集中在450μm高的微针针体上,微针穿刺皮肤后恰好到达真皮层并且在皮肤上形成约250μm深的微通道,微针针体能在5 min中内迅速溶解,为麻醉微针透皮给药实际应用提供一定技术依据。

To understand the preparation process and skin-puncturing effect of microneedles with stratified solubility for efficient use of lidocaine,the polymer microneedles were prepared by two casting methods using polydimethylsiloxane as a negative model and the polyvinyl alcohol/sodium hyaluronate/polyvinylpyrrolidone compound as a composite matrix.The morphology of the resulting polymer microneedles was observed by a microscope,and their height was measured.The puncturing test was conducted on the abdominal skin of a mouse,and then the puncturing effect of microneedles was investigated upon the obtained frozen sections.The experimental results indicated that the lidocaine-containing polymer microneedles achieved a formation rate of 100%,and lidocaine was mainly distributed in the needle bodies of the microneedles at a height of 450μm.The microneedles were able to penetrate the skin just after reaching the dermis layer by giving a channel with a depth of about 250μm through the skin.In addition,90 wt%of the needle bodies dissolved rapidly within 5 min,and the molding cycle was shortened within 4 hours.