Luo Yali, Yao Xinjian, Yuan Jinfang, Ding Tao, Gao Qingyu
Institute of Fine Chemical and Engineering, Henan University, Kaifeng, Henan 475001, P R China.
Colloids Surf B Biointerfaces. 2009 Feb 1;68(2):218-24. doi: 10.1016/j.colsurfb.2008.10.014. Epub 2008 Nov 5.
Block copolymers, poly(N-vinylprrolidone)-block-poly(styrene-alter-maleic anhydride) (PVP-b-PSMA) and poly(N-vinylprrolidone)-block-poly(N,N-dimethylaminoethyl methacrylate) (PVP-b-PDMAEMA), were synthesized by reversible addition- fragmentation chain transfer (RAFT) polymerization. In aqueous media, this a pair of oppositely-charged diblock copolymers could self-assemble into stable and narrow distribution polyion complex micelles (PICMs). Transmission electron micrographs (TEM) and dynamic light scattering (DLS) analysis showed that the micelles to be spherically shaped with mean hydrodynamic diameter around 70nm. In addition, the PICMs display ability to response to external stimuli. All of theses features are quite feasible for utilizing it as a novel intelligent drug delivery system. In order to assess its application in biomedical area, release profiles of coenzyme A (Co A) from PICMs were studied under both simulated gastric and intestinal pH conditions. The release was much quicker in pH 7.4 buffer than in pH 2.0 solution. Based on these results, these PICMs could be a potential pH-sensitive carrier for colon-specific drug delivery system.
通过可逆加成-断裂链转移(RAFT)聚合法合成了嵌段共聚物,聚(N-乙烯基吡咯烷酮)-嵌段-聚(苯乙烯-alt-马来酸酐)(PVP-b-PSMA)和聚(N-乙烯基吡咯烷酮)-嵌段-聚(甲基丙烯酸N,N-二甲基氨基乙酯)(PVP-b-PDMAEMA)。在水性介质中,这一对带相反电荷的二嵌段共聚物可自组装成稳定且分布窄的聚离子复合胶束(PICM)。透射电子显微镜(TEM)和动态光散射(DLS)分析表明,胶束呈球形,平均流体动力学直径约为70nm。此外,PICM表现出对外部刺激的响应能力。所有这些特性使其作为一种新型智能药物递送系统具有很大可行性。为了评估其在生物医学领域的应用,研究了在模拟胃和肠pH条件下辅酶A(CoA)从PICM中的释放曲线。在pH 7.4缓冲液中的释放比在pH 2.0溶液中快得多。基于这些结果,这些PICM可能是用于结肠特异性药物递送系统的潜在pH敏感载体。