Greco Francesca, Vicent Maria J
School of Pharmacy, University of Reading, Whiteknights, PO BOX 224, Reading RG6 6AD, Berkshire, UK.
Front Biosci. 2008 Jan 1;13:2744-56. doi: 10.2741/2882.
Polymer conjugates are nano-sized, multi-component constructs already in the clinic as anticancer compounds, both as single agents or as elements of combinations. They have the potential to improve pharmacological therapy of a variety of solid tumors. Polymer-drug conjugation promotes passive tumor targeting by the enhanced permeability and retention (EPR) effect and allows for lysosomotropic drug delivery following endocytic capture. In the first part of this review, we analyze the promising results arising from clinical trials of polymer-bound chemotherapy. The experience gained on these studies provides the basis for the development of a more sophisticated second-generation of polymer conjugates. However, many challenges still lay ahead providing scope to develop and refine this field. The ''technology platform'' of polymer therapeutics allows the development of both new and exciting polymeric materials, the incorporation of novel bioactive agents and combinations thereof to address recent advances in drug therapy. The rational design of polymer drug conjugates is expected to realize the true potential of these "nanomedicines".
聚合物缀合物是纳米尺寸的多组分构建体,已作为抗癌化合物应用于临床,既可以作为单一药物,也可以作为联合用药的成分。它们有潜力改善多种实体瘤的药物治疗。聚合物-药物缀合通过增强的渗透和滞留(EPR)效应促进被动肿瘤靶向,并允许在胞吞捕获后进行溶酶体亲和性药物递送。在本综述的第一部分,我们分析了聚合物结合化疗临床试验中产生的有前景的结果。这些研究获得的经验为开发更复杂的第二代聚合物缀合物提供了基础。然而,仍有许多挑战摆在面前,为该领域的发展和完善提供了空间。聚合物治疗的“技术平台”允许开发新型且令人兴奋的聚合物材料,纳入新型生物活性剂及其组合,以应对药物治疗的最新进展。聚合物药物缀合物的合理设计有望实现这些“纳米药物”的真正潜力。