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用于抗癌治疗的自组装药物偶联物。

Self-assembly drug conjugates for anticancer treatment.

作者信息

Fumagalli Gaia, Marucci Cristina, Christodoulou Michael S, Stella Barbara, Dosio Franco, Passarella Daniele

机构信息

Dipartimento di Chimica, Università degli Studi di Milano, Via Golgi 19, 20133 Milano, Italy.

Dipartimento di Scienza e Tecnologia del Farmaco, Università degli Studi di Torino, Via Giuria 9, 10125 Torino, Italy.

出版信息

Drug Discov Today. 2016 Aug;21(8):1321-9. doi: 10.1016/j.drudis.2016.06.018. Epub 2016 Jun 18.

Abstract

Self-assembly drug conjugate preparation is a promising approach to improve activity and penetration through physiological barriers of potent small molecules, as well as to reduce any side effects. Drug conjugates can self-assemble in water to form nanoparticles (NPs) that offer several advantages because: (i) they are easy to obtain; (ii) they can reach high local drug concentration in tumor tissues; and (iii) they can reduce the side effects of drugs. All these factors improve drug pharmacokinetic properties. Here, we have reviewed the scope of nanotechnology-based self-assembly drug delivery approaches focusing on prodrugs able to form NPs by self-assembly; we have also summarized the current perspective and challenges facing the successful treatment of cancer.

摘要

自组装药物缀合物的制备是一种很有前景的方法,可提高强效小分子的活性并穿透生理屏障,同时减少任何副作用。药物缀合物可在水中自组装形成纳米颗粒(NPs),具有以下几个优点:(i)易于制备;(ii)可在肿瘤组织中达到高局部药物浓度;(iii)可减少药物的副作用。所有这些因素都改善了药物的药代动力学性质。在此,我们综述了基于纳米技术的自组装药物递送方法的范围,重点关注能够通过自组装形成纳米颗粒的前药;我们还总结了当前癌症成功治疗面临的前景和挑战。

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