Synthesis, drug release and targeting behaviors of Novel Folated Pluronic F87/poly(lactic acid) block copolymer
Synthesis, drug release and targeting behaviors of Novel Folated Pluronic F87/poly(lactic acid) block copolymer
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新型叶酸Pluronic F87/聚乳酸嵌段共聚物的合成、药物释放及靶向行为
DOI：
10.1016/j.eurpolymj.2015.05.003
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发表时间：
2015-07
影响因子：
6
通讯作者：
Li Yu Ping
中科院分区：
文献类型：
--
作者：
Xiong Xiang Yuan;Qin Xiang;Li Zi Ling;Gong Yan Chun;Li Yu Ping
通过两步反应合成了新型叶酸Pluronic F87/聚乳酸嵌段共聚物（FA-F87-PLA）。用荧光光谱、动态光散射和透射电镜研究了FA-F87-PLA嵌段共聚物在水溶液中的自组装行为。FA-F87-PLA纳米粒的形貌为球形胶束。在FA-F87-PLA纳米颗粒中负载的紫杉醇（PTX）在前11小时显示初始突释，随后缓慢释放。通过3-（4，5-二甲基噻唑-2-基）-2，5-二苯基溴化四氮唑（MTT）试验研究FA-F87-PLA纳米粒对OVCAR-3（叶酸受体阳性）的体外靶向行为。MTT结果表明，FA-F87-PLA纳米粒表面的叶酸基团与OVCAR-3细胞表面的叶酸受体特异性靶向相互作用，FA-F87-PLA纳米粒中的PTX对OVCAR-3细胞的抗癌作用强于非靶向PLA-F87-PLA纳米粒中的PTX。通过荧光显微镜（FM）技术进一步证实了FA-F87-PLA纳米粒的靶向性。还使用三重标记方法研究了FA-F87-PLA纳米粒的细胞内分布。观察到FA-F87-PLA纳米颗粒主要位于OVCAR-3细胞的细胞质内。
Novel Folated Pluronic F87/poly(lactic acid) block copolymer (FA-F87–PLA) was synthesized by two step reactions. The self-assembling behavior of FA-F87–PLA block copolymer in aqueous solutions was examined by fluorescence measurement, Dynamic Light Scattering (DLS) and Transmission Electron Microscopic (TEM) techniques. The morphology of FA-F87–PLA nanoparticles was found to be spherical micelles. Paclitaxel (PTX) loaded in FA-F87–PLA nanoparticles shows an initial burst release in the first 11 h and followed by a slow release. The in vitro targeting behavior of FA-F87–PLA nanoparticles against OVCAR-3 (folate receptor positive) was investigated by 3-(4,5-Dimethylthiazol-2-yl)-2,5-diphenyl tetrazolium bromide (MTT) tests. MTT results show that the anticancer effect of PTX in FA-F87–PLA nanoparticle over OVCAR-3 cells was stronger than that of PTX in nontargeted PLA–F87–PLA nanoparticle under the specific targeting interaction between folate groups on the surface of FA-F87–PLA nanoparticles and folate receptor on the surface of OVCAR-3 cells. The targeting behaviors of FA-F87–PLA nanoparticles were further confirmed by fluorescence microscopy (FM) technique. The intracellular distribution of FA-F87–PLA nanoparticles was also studied using a triple-labeling method. It was observed that FA-F87–PLA nanoparticles are mainly localized within the cytoplasm of OVCAR-3 cells.
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DOI：
10.1016/j.colsurfb.2012.07.030
发表时间：
2013-02
期刊：
Colloids and surfaces. B, Biointerfaces
影响因子：
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作者：
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DOI：
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发表时间：
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期刊：
European journal of pharmaceutical sciences : official journal of the European Federation for Pharmaceutical Sciences
影响因子：
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DOI：
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发表时间：
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期刊：
Colloids and surfaces. B, Biointerfaces
影响因子：
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影响因子：
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