寡肽药物结合物用作前药在药物递送中的应用
摘 要 临床实践证明，治疗性化合物的共价修饰是设计出治疗功效增强的前药的一种行之有效的策略。这种前药策略依赖于药代动力学性质和给药途径优于其母体药物的的修饰药物。自组装前药代表了一类新兴的治疗剂，能够自发地在水溶液中结合成明确的超分子纳米结构，其中包含寡肽药物结合物。除了改善药物溶解性、延长其在体内作用时间等优点之外，以寡肽作为靶向配体构建的肿瘤靶向药物对实现抗肿瘤药物的靶向递送提供了一条新的途径。在该综述中，我们将讨论寡肽药物结合物的发展情况，概述前药设计的指导原则，总结其在药物靶向递送中的应用，为该领域的未来发展提供借鉴。
关键词 前药设计；靶向递送；自组装前药；寡肽药物结合物
AbstractCovalent modification of therapeutic compounds is a clinically proven strategy to devise prodrugs with enhanced treatment efficacies. This prodrug strategy relies on the modified drugs that possess advantageous pharmacokinetic properties and administration routes over their parent drug. Self-assembling prodrugs which also contains polypeptide-drug conjugates represent an emerging class of therapeutic agents capable of spontaneously associating into well-defined supramolecular nanostructures in aqueous solutions. In addition to improving the solubility of the drug and prolonging the time of its action in vivo, the tumor-targeted drugs constructed using the peptide as a targeting ligand are used for the realization of targeted delivery of anti-neoplastic drugs. In this review, we will discuss the development of polypeptide-drug conjugates, provide an overview of the guiding principles in the molecular design of each prodrug group, summarize its application in drug targeted delivery and provide a reference for the future development of the field.
Key Words Prodrug Design;Targeted Delivery; Self-assembling Prodrugs;Peptide-drug Conjugates
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