Zhang Li-Qiao, Luan Li-Biao, Wu Yan, Wang Dong-Mei
Department of Pharmaceutics of China Pharmaceutical University, Nanjing 211198, China.
Zhongguo Zhong Yao Za Zhi. 2013 Jul;38(13):2109-13.
To synthetize 3-carboxypropyl-triphenylphosponium bromide-polycaprolacton-CTPP-PEG-PC, and prepare curcumin CTPP-PEG-PCL micelles by using the self-assembled emulsion solvent evaporation method, in order to determine the critical micelle concentration (CMC) with the pyrene fluorescent probe technology, detect the particle size, entrapment efficiency (%), morpheme and in vitro release rate, and evaluate the cytotoxicity of hepatic stellate cells with MTT assay. The structure of CTPP-PEG-PCL had been identified by 1H-NMR spectra. Specifically, the CMC of polymer was 2.25 mg x L(-1), the average size was 190 nm, the drug content was (0.66 +/- 0.008) g x L(-1), and the entrapment efficiency was (94 +/- 0.6)%. The in vitro release results showed curcumin micelles had a significant higher inhibition ratio in the growth of hepatic stellate cells than crude curcumin (P < 0.05). This suggested that CTPP-PEG-PCL micelles feature low CMC, high encapsulation efficiency and notable inhibition effect in growth of hepatic stellate cells.
合成3-羧丙基-三苯基溴化膦-聚己内酯-CTPP-聚乙二醇-聚己内酯（CTPP-PEG-PCL），采用自组装乳化溶剂蒸发法制备姜黄素CTPP-PEG-PCL胶束，以芘荧光探针技术测定临界胶束浓度（CMC），检测粒径、包封率（%）、形态和体外释放率，并用MTT法评估肝星状细胞的细胞毒性。通过1H-NMR光谱鉴定了CTPP-PEG-PCL的结构。具体而言，聚合物的CMC为2.25 mg·L(-1)，平均粒径为190 nm，药物含量为(0.66±0.008) g·L(-1)，包封率为(94±0.6)%。体外释放结果表明，姜黄素胶束对肝星状细胞生长的抑制率显著高于姜黄素粗品（P<0.05）。这表明CTPP-PEG-PCL胶束具有低CMC、高包封效率和对肝星状细胞生长显著的抑制作用。
