Department of Chemistry, State Key Laboratory of Elemento-Organic Chemistry, Collaborative Innovation Center of Chemical Science and Engineering and ‡Department of Biochemistry and Molecular Biology, College of Life Sciences, Nankai University , Tianjin 300071, P. R. China.
J Med Chem. 2013 Dec 12;56(23):9725-36. doi: 10.1021/jm4014168. Epub 2013 Nov 22.
A series of conjugated hyaluronic acid particles (HAP), composed of a hydrophobic anticancer drug core and hydrophilic cyclodextrin/hyaluronic acid shell, were prepared through self-assembling and characterized by (1)H NMR titration, electron microscopy, zeta potential, and dynamic light-scattering experiments. The nanometer-sized HAP thus prepared was biocompatible and biodegradable and was well-recognized by the hyaluronic acid receptors overexpressed on the surface of cancer cells, which enabled us to exploit HAP as an efficient targeted delivery system for anticancer drugs. Indeed, HAP exhibited anticancer activities comparable to the commercial anticancer drug cisplatin but with lower side effects both in vitro and in vivo.
一系列的共轭透明质酸颗粒（HAP），由疏水性抗癌药物核心和亲水环糊精/透明质酸壳组成，通过自组装制备，并通过（1）H NMR 滴定、电子显微镜、Zeta 电位和动态光散射实验进行了表征。所制备的纳米级 HAP 具有生物相容性和可生物降解性，并且被癌细胞表面过度表达的透明质酸受体很好地识别，这使我们能够利用 HAP 作为抗癌药物的有效靶向递送系统。事实上，HAP 在体外和体内均表现出与商业抗癌药物顺铂相当的抗癌活性，但副作用较低。
