DSAPM Lab and PCFM Lab, Institute of Polymer Science, School of Chemistry and Chemical Engineering, Sun Yat-Sen University, Guangzhou 510275, China.
J Colloid Interface Sci. 2013 Sep 1;405:305-11. doi: 10.1016/j.jcis.2013.05.017. Epub 2013 May 28.
To develop a multifunctional polymeric carrier for gene and drug co-delivery, a new cyclodextrin derivative containing poly(L-lysine) dendrons was prepared by the click conjugation of per-6-azido-β-cyclodextrin with propargyl focal point poly(L-lysine) dendron of third generation and then characterized by FTIR, (1)H NMR, and GPC analyses. It was found that such a conjugate could form colloidally stable nanocomplexes with plasmid DNA in aqueous system and exhibited high gene transfection efficiency. Moreover, it could load efficiently methotrexate drug with anticancer activity and showed a sustained release behavior. Different from commonly used amphiphilic copolymers with cationic character, the as obtained cyclodextrin derivative may be used directly for the combinatorial delivery of nucleic acid and lipophilic anticancer drugs without a complicated micellization process.
为了开发用于基因和药物共递药的多功能聚合物载体，通过点击反应将含有聚（L-赖氨酸）树枝状大分子的第三代炔丙基焦点聚（L-赖氨酸）树枝状大分子与六-叠氮-β-环糊精连接，制备了一种新的环糊精衍生物，然后通过 FTIR、（1）H NMR 和 GPC 分析进行了表征。结果表明，该化合物在水相中可以与质粒 DNA 形成胶体稳定的纳米复合物，并表现出高的基因转染效率。此外，它可以有效地装载具有抗癌活性的甲氨蝶呤药物，并表现出持续释放行为。与常用的具有阳离子特性的两亲性共聚物不同，所得到的环糊精衍生物可直接用于核酸和疏水性抗癌药物的组合递药，而无需复杂的胶束化过程。
