靶向肿瘤纳米晶体的研究进展

纳米晶体是以少量表面活性剂或高分子聚合物为稳定剂,将难溶性药物粒子分散于水或油中形成的纳米级（1~1 000 nm）分散体系。纳米晶体含药量高,制备工艺简单成熟。目前,已上市的24个纳米晶体制剂主要集中在改善难溶性药物溶解性以及提高生物利用度上。近几年来,关于纳米晶体通过控制粒径或表面修饰实现靶向给药的研究逐渐成为热点。本文主要介绍了用于延长纳米晶体体内循环时间、增加对肿瘤细胞的亲和力、实现对内外刺激的响应的3种靶向策略,并探讨了纳米晶体技术应用于靶向抗肿瘤药物存在的瓶颈,为纳米晶体制剂的开发提供参考。

Advances in tumor targeted nanocrystals

Nanocrystals are nanoscale (1-1000 nm) dispersion systems in which small numbers of surfactants or polymers are used as stabilizers to disperse insoluble drug particles in water or oil. Nanocrystals enjoy not only high drug content, but also a simple and mature preparation process. At present, 24 nanocrystals products that have been marketed mainly focus on enhancing the solubility and bioavailability of poorly soluble drugs. And recent years have witnessed an increasing number of research reports on target drug delivery of nanocrystals through particle size control and surface modification. This paper mainly introduces three targeting strategies for prolonging the in vivo circulation time of nanocrystals, increasing the affinity for tumor cells and achieving the response to internal and external stimuli, and discusses the current challenges in the application of nanocrystal technology to targeted anti-tumor drugs.