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大分子药物的肿瘤靶向递送机制,包括实体瘤中的EPR效应及原型聚合物药物SMANCS的临床概述。

Mechanism of tumor-targeted delivery of macromolecular drugs, including the EPR effect in solid tumor and clinical overview of the prototype polymeric drug SMANCS.

作者信息

Maeda H, Sawa T, Konno T

机构信息

Department of Microbiology, Kumamoto University School of Medicine, 860-0811, Kumamoto, Japan.

出版信息

J Control Release. 2001 Jul 6;74(1-3):47-61. doi: 10.1016/s0168-3659(01)00309-1.

Abstract

This review article describes three aspects of polymeric drugs. The general mechanism of the EPR (enhanced permeability and retention) effect and factors involved in the effect are discussed, in view of the advantages of macromolecular therapeutics for cancer treatment, which are based on the highly selective EPR-related delivery of drug to tumor. Also described are advantages of more general water-soluble polymeric drugs as primary anticancer agents, using SMANCS as an example. Last, SMANCS/Lipiodol is discussed with reference to the type of formulation for arterial injection with most pronounced tumor selective delivery, as well as its advantages, precautions, and side effects from the clinical standpoint.

摘要

这篇综述文章描述了聚合物药物的三个方面。鉴于基于与EPR(增强的通透性和滞留性)相关的药物向肿瘤的高度选择性递送的大分子疗法在癌症治疗中的优势,讨论了EPR效应的一般机制以及涉及该效应的因素。还以SMANCS为例,描述了更通用的水溶性聚合物药物作为主要抗癌剂的优势。最后,从临床角度讨论了SMANCS/碘油,涉及具有最显著肿瘤选择性递送的动脉注射制剂类型及其优势、注意事项和副作用。

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