Fumagalli Gaia, Marucci Cristina, Christodoulou Michael S, Stella Barbara, Dosio Franco, Passarella Daniele
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.
Drug Discov Today. 2016 Aug;21(8):1321-9. doi: 10.1016/j.drudis.2016.06.018. Epub 2016 Jun 18.
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.
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。
