基于壳聚糖的可控缓释型微针制备与性能评价  

Preparation and performance evaluation of controlled-release chitosan-based microneedles

作　　者：朱龙 庄俭[1] 赵泽伟 刘俸溢 薛庆隆 孙靖尧 黄尧 许红[1] ZHU Long;ZHUANG Jian;ZHAO Zewei;LIU Fengyi;XUE Qinglong;SUN Jingyao;HUANG Yao;XU Hong(Institute of Plastic Machinery and Plastic Engineering(IPME),Beijing University of Chemical Technology,Beijing 100029,China)

机构地区：[1]北京化工大学塑料机械与塑料工程研究所,北京100029

出　　处：《生物工程学报》2022年第9期3478-3488,共11页Chinese Journal of Biotechnology

摘　　要：在临床应用上,一种能够持续递送药物的微针(microneedle,MN)系统对于一些疫苗、激素类药物的递送具有重要价值。本文研究设计了一种基于壳聚糖的可控缓释型微针阵列(PVA/CS-MN),将微针贴片与药物相结合用于药物的可控长效缓释。重点研究了PVA/CS-MN的制备优化工艺,并对MN阵列外观形貌、力学性能、溶解与溶胀性能以及体外刺入性能进行了表征。实验结果表明,使用最优工艺制备的PVA/CS-MN具有良好的形貌以及力学性能,可以顺利在皮肤上打开微通道,并实现可控的溶解与溶胀功能。同时,体外透皮扩散实验表明,以抗坏血酸(L-ascorbic acid)为模型药物制备的Vc-PVA/CS-MN在1 h内即释放了约57%的药物,随后12 h内缓慢释放了约66.7%的药物,7 d后最终释放了92%的药物。PVA/CS-MN具备可控的缓释特性以及优良的药物递送效率,为药物的持续透皮递送提供了一个新选择。In clinical application,a microneedle system that continuously delivers drugs is of great value for the delivery of some vaccines and hormone drugs.In this study,a controlled-release chitosan-based microneedle array(PVA/CS-MN)was designed,combining microneedle patches with drugs for controlled-release of drugs.Here we report the optimization of the preparation process of PVA/CS-MN.The appearance,morphology,mechanical properties,dissolution and swelling properties,and in vitro penetration properties of the MN arrays were characterized.The PVA/CS-MN prepared by the optimal process showed good morphology and mechanical properties.PVA/CS-MN can smoothly open microchannels on the skin and achieve controllable dissolution and swelling functions.Ascorbic acid(L-ascorbic acid)was used as a model drug to prepare a Vc-PVA/CS-MN.In vitro transdermal diffusion experiments showed that the Vc-PVA/CS-MN released about 57%of the drug within 1 h.About 66.7%of the drug was slowly released within 12 h,and a total of 92%of the drug was released after 7 days.The controllable sustained-release properties and excellent drug delivery efficiency of PVA/CS-MN provide a new option for sustained transdermal drug delivery.

关 键 词：壳聚糖 缓释型微针 刺入性能 溶胀性能 释药效果 

分 类 号：TQ460.4[化学工程—制药化工]