Li Guiying, Song Sen, Zhang Ting, Qi Minyi, Liu Junshen
College of Chemistry and Materials Science, Ludong University, Yantai 264025, China.
Int J Biol Macromol. 2013 Nov;62:203-10. doi: 10.1016/j.ijbiomac.2013.08.041. Epub 2013 Aug 31.
In this paper, pH-sensitive polyelectrolyte complex micelles assembled from two oppositely charged graft copolymers chitosan-g-poly(N-isopropylacrylamide) (CS-g-PNIPAM) and sodium alginate-g-poly(N-isopropylacrylamide-co-N-vinyl-pyrrolidone) [ALG-g-P(NIPAM-co-NVP)] were prepared for controlled release of 5-fluorouracil (5-FU). The polyelectrolyte complex micelles showed a narrow size distribution with core-shell structure, where the core formed from positively charged CS and negatively charged ALG by electrostatic interactions. The hydrogen bonding interactions between micelles and 5-FU improved the drug loading. Changing temperature or pH, a controlled drug release was observed. Glutaraldehyde, as a chemical cross-linking agent, was used to improve the micelles stability and decrease the initial burst release. Cytotoxicity assays showed that drug-loaded micelles retained high cell inhibition efficiency in Hela cells. These novel complex micelles with environmentally sensitive properties are expected to be useful in the field of intelligent drug delivery system.
本文制备了由两种带相反电荷的接枝共聚物壳聚糖 - g - 聚(N - 异丙基丙烯酰胺)(CS - g - PNIPAM)和海藻酸钠 - g - 聚(N - 异丙基丙烯酰胺 - 共 - N - 乙烯基吡咯烷酮)[ALG - g - P(NIPAM - 共 - NVP)]组装而成的pH敏感型聚电解质复合胶束,用于5 - 氟尿嘧啶(5 - FU)的控释。聚电解质复合胶束呈现出具有核壳结构的窄尺寸分布,其中核由带正电荷的CS和带负电荷的ALG通过静电相互作用形成。胶束与5 - FU之间的氢键相互作用提高了药物负载量。改变温度或pH值时,可观察到药物的控释。戊二醛作为化学交联剂,用于提高胶束稳定性并减少初始突释。细胞毒性试验表明,载药胶束在Hela细胞中保持了较高的细胞抑制效率。这些具有环境敏感特性的新型复合胶束有望在智能药物递送系统领域发挥作用。