共价修饰策略的局部麻醉剂药物递送系统研究进展  

Research progress on local anesthetic drug delivery systems based on covalent modification strategies

作　　者：姚佳星 刘自福 郑月钦 YAO Jia-xing;LIU Zi-fu;ZHENG Yue-qin(State Key Laboratory of Natural Medicine,Center of Drug Discovery,China Pharmaceutical University,Nanjing 211198,China)

机构地区：[1]中国药科大学新药研究中心,多靶标天然药物国家重点实验室,江苏南京211198

出　　处：《药学学报》2024年第12期3215-3221,共7页Acta Pharmaceutica Sinica

基　　金：中国药科大学多靶标天然药物全国重点实验室专项计划。

摘　　要：本综述介绍了共价修饰策略在局部麻醉剂药物递送系统中的研究进展。局部麻醉剂作为一种常用的多模式镇痛药物,在临床应用中存在作用时间有限和潜在毒性的限制。为了达到延长镇痛效果、减轻全身毒性的目的,研究者们致力于开发具有持久剂量控释功能的局部麻醉剂缓释制剂。在局部麻醉剂的递送方面,共价修饰策略是一种关键的方法。通过药物与大分子载体的共价键结合,能够提高药物的稳定性、靶向性和递送效率。大分子前药可以调节药物的动力学过程,使药物以活性成分形式释放,并实现更好的治疗效果。近年来,刺激响应性大分子前药成为研究热点,对于局部麻醉剂药物递送系统,大分子前药的刺激响应性能可以在内外刺激条件下迅速释放药物,并在血液循环和正常组织中维持低毒和高效性。这些新兴的研究方向为延长局部麻醉剂的镇痛效果、减轻全身毒性提供了重要的指导,并为开发更有效的药物递送系统提供了新的思路。This review introduced the research progress of covalent modification strategies in local anesthetic drug delivery systems.As a commonly used and multimodal analgesic drug,local anesthetics have limited duration of action and potential toxicity in clinical application.In order to prolong the analgesic effect and reduce systemic toxicity,researchers are committed to the development of sustained-release local anesthetics with long-lasting dosecontrolled-release functions.When it comes to the delivery of local anesthetics,the covalent modification strategy is a key approach.By covalently binding drugs to large molecule carriers,covalent modification strategies can improve drug stability,targeting and delivery efficiency.Macromolecular prodrugs can modulate the kinetic process of the drug,so that the drug is released in the form of the active ingredient and achieve better therapeutic effects.In recent years,stimulus-responsive macromolecular prodrugs have become a research hotpot for local anesthetic drug delivery systems,and the stimulus-responsive performance of macromolecular prodrugs can rapidly release drugs under internal and external stimulus conditions,and maintain low toxicity and high efficiency in blood circulation and normal tissues.These emerging research directions provide important guidance for prolonging the analgesic effect of local anesthetics and reducing systemic toxicity,and provide new idea for the development of more effective drug delivery systems in the future.

关 键 词：局部麻醉剂 药物递送系统 共价修饰 大分子前药 刺激响应性大分子前药 

分 类 号：R943[医药卫生—药剂学]