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摘要: 减少用药次数、延长术后镇痛时间是临床局部麻醉的重要需求。然而，无论是当前临床使用的局麻药，还是生物毒素类潜在新型麻醉药均存在时效较短的问题。利用脂质体、聚合物微球等药物载体装载局麻药进行控释，可实现药物的长效、按需释放，从而满足临床需求。本文简要概述可用于局麻药控释的药物载体，并介绍具有代表性的药物控释体系的设计、功能及其用于局部麻醉的最新研究进展，同时对此研究领域的挑战及未来前景进行讨论。Abstract: Reducing the drug administration times and prolonging the postoperative analgesia duration are important requirements of clinical local anesthesia. However, both local anesthetics currently used in the clinic and potentially new anesthetic drugs such as biological toxins have limited pharmaceutical effect. Biomaterials such as liposomes and polymeric microspheres can be designed to load local anesthetics to achieve a prolonged duration and on-demand drug release, accordingly satisfying clinical needs. In this review, we briefly summarized the recent developments in the design of drug delivery systems for controlled release of local anesthetics, and introduced the design principle, the function of several representative drug controlled release systems, and their applications in local anesthesia. We also discussed the challenges and future perspectives in this field.
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Key words:
- drug carrier /
- local anesthesia /
- controlled release /
- responsive release /
- long-term efficacy
作者贡献：龙凯负责查阅文献和论文撰写；曹佩负责论文撰写和修订；季天骄负责论文主题确定、论文修订。利益冲突：所有作者均声明不存在利益冲突 -
图 2 基于仿生思路设计的新型局麻药缓释体系
A.新型局麻药河豚毒素及其与钠离子通道蛋白结合区域；B.含有与河豚毒素结合序列的两亲性多肽分子序列(载体分子设计)；C.两亲性载体分子自组装载药示意图及载体自组装透射电镜形貌(纳米纤维)；D.不同疏水基团(C12、C18、疏水氨基酸等)修饰的两亲性多肽载体对河豚毒素的缓释情况；E.优选组载体麻醉效力及对应的剂量
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