标题：Galactose-Decorated pH-Responsive Nanogels for Hepatoma-Targeted Delivery of Oridonin
作者：Cunxian Duan;Jian Gao;Dianrui Zhang
作者机构：[Duan, C] Department of Pharmaceutics, Jinan 250012, China;[ Gao, J] Department of Natural Product Chemistry, Jinan 250012, China;[ Zhang, D] Departme 更多
通讯作者地址：[Zhang, DR]Shandong Univ, Sch Pharmaceut Sci, Dept Pharmaceut, Jinan 250012, Peoples R China.
摘要：Nanogels based on the polymers of galactosylated chitosan-graft-poly (N-isopropylacrylamide) (Gal-CS-g-PNIPAm) were used as carriers of oridonin (ORI) for tumor targeting. Three ORI-loaded nanogels with various degrees of galactose substitution were prepared, and their characteristics were evaluated. The release behavior of ORI from these nanogels was pH-dependent, and the release could be accelerated under mildly acidic conditions. The cytotoxicity of ORI-loaded nanogels was pH-sensitive. ORI-loaded nanogels exhibited a higher antitumor activity than drug-loaded nanogels without galactosylation, and the anticancer activity increased in relation to increases in the number of galactose moieties of the nanogels in HepG2 cells. In contrast, the cytotoxicity of ORI-loaded nanogels against MCF-7 cells decreased compared with that of drug-loaded nanogels without galactosylation. Results demonstrated that these nanogels could enhance the uptake of ORI into HepG2 cells via asialoglycoprotein receptor-mediated endocytosis. These galactose-decorated pH-responsive nanogels were well-suited for targeted drug delivery to liver cancer cells.