基于交联透明质酸的微针制备及性能

Preparation and Performance of Microneedles Based on Cross-Linked Hyaluronic Acid

新型水凝胶微针具有安全包裹多相药物、药物持续、可控释放等优点,在微针透皮给药领域极具应用潜力。文中重点研究了交联透明质酸微针贴片的优化工艺,并对微针贴片进行了性能评价。在碱性条件下使用1,4-丁二醇二缩水甘油醚(BDDE)为交联剂对透明质酸进行交联,利用微浇注法制备交联透明质酸微针(cHA-MN),并优化其工艺。对所制备的微针贴片进行了外观形貌、力学性能、体外刺入性能及溶胀性能表征,验证其能否满足使用要求。实验结果表明,使用最优工艺制备的交联透明质酸微针贴片力学性能优良,可以顺利刺破皮肤,并实现溶胀功能。使用制备的微针搭载2.5%的右旋布洛芬药物,体外透皮扩散结果表明,微针在0~6 h释放出约38%药物,随后以一定速度缓慢释放至42 h,累计释放率约90%。

Novel hydrogel microneedles have the advantages of safely loading multiphase drugs, sustained release, and controlled release. It has great potential application in the field of microneedle transdermal drug delivery. In this paper, the optimization process of the cross-linked hyaluronic acid microneedle patch was studied, and the performance of the microneedle patch was evaluated. Under alkaline conditions, hyaluronic acid was cross-linked with 1,4-butanediol diglycidyl ether(BDDE). The cross-linked hyaluronic acid microneedles(cHA-MN) were fabricated by micro-casting method, and the process was optimized. To verify whether the prepared microneedle patch can meet the requirements of use, its appearance, mechanical properties, in vitro insertion properties, and swelling properties were characterized. The results show that the cHA-MN patch prepared by the optimal process has excellent mechanical properties, which allows it to be inserted into the skin smoothly. In addition, the swelling function can also be realized. This provides the possibility for the subsequent use of cHA-MN for continuous drug delivery. The prepared microneedles were loaded with 2.5% dexibuprofen. The results of in vitro transdermal diffusion show that the microneedles release about 38% of the drug in 0~6 h, and then slowly release to 42 h, with a cumulative release rate of about 90%.