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嵌段共聚物胶束:制备、表征及其在药物递送中的应用。

Block copolymer micelles: preparation, characterization and application in drug delivery.

作者信息

Gaucher Geneviève, Dufresne Marie-Hélène, Sant Vinayak P, Kang Ning, Maysinger Dusica, Leroux Jean-Christophe

机构信息

Canada Research Chair in Drug Delivery, Faculty of Pharmacy, University of Montreal, Downtown Station, Canada.

出版信息

J Control Release. 2005 Dec 5;109(1-3):169-88. doi: 10.1016/j.jconrel.2005.09.034. Epub 2005 Nov 11.

Abstract

Block copolymer micelles are generally formed by the self-assembly of either amphiphilic or oppositely charged copolymers in aqueous medium. The hydrophilic and hydrophobic blocks form the corona and the core of the micelles, respectively. The presence of a nonionic water-soluble shell as well as the scale (10-100 nm) of polymeric micelles are expected to restrict their uptake by the mononuclear phagocyte system and allow for passive targeting of cancerous or inflamed tissues through the enhanced permeation and retention effect. Research in the field has been increasingly focused on achieving enhanced stability of the micellar assembly, prolonged circulation times and controlled release of the drug for optimal targeting. With that in mind, our group has developed a range of block copolymers for various applications, including amphiphilic micelles for passive targeting of chemotherapeutic agents and environment-sensitive micelles for the oral delivery of poorly bioavailable compounds. Here, we propose to review the innovations in block copolymer synthesis, polymeric micelle preparation and characterization, as well as the relevance of these developments to the field of biomedical research.

摘要

嵌段共聚物胶束通常是由两亲性或带相反电荷的共聚物在水性介质中自组装形成的。亲水嵌段和疏水嵌段分别形成胶束的冠层和核层。预计非离子水溶性外壳的存在以及聚合物胶束的尺寸(10 - 100纳米)会限制单核吞噬细胞系统对它们的摄取,并通过增强渗透和滞留效应实现对癌组织或炎症组织的被动靶向。该领域的研究越来越集中于实现胶束组装体的稳定性增强、循环时间延长以及药物的控释以实现最佳靶向。考虑到这一点,我们团队已开发出一系列用于各种应用的嵌段共聚物,包括用于化疗药物被动靶向的两亲性胶束以及用于口服递送生物利用度差的化合物的环境敏感型胶束。在此,我们提议综述嵌段共聚物合成、聚合物胶束制备与表征方面的创新,以及这些进展与生物医学研究领域的相关性。

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