姜黄素CTPP-PEG-PCL胶束的制备及体外评价

Preparation and in vitro evaluation of curcumin CTPP-PEG-PCL micelles

该研究合成了材料3-羧丙基-三苯基溴化鏻-聚乙二醇-聚己内酯(CTPP-PEG-PCL),并且采用自组装溶剂挥发法制备载姜黄素CTPP-PEG-PCL胶束,芘荧光光谱法测定临界胶束浓度(critical micelle concentration,CMC),考察粒径、包封率、形态、体外释放度;采用MTT实验进行肝星状细胞毒性评价。所得材料CTPP-PEG-PCL经1H NMR表征确证其结构,CMC为2.252 mg.L-1,胶束粒径约为190 nm,含药量为(0.66±0.008)g.L-1,包封率(94±0.6)%,体外释放显示缓释特性,姜黄素胶束对肝星状细胞的生长抑制率显著高于姜黄素原料药(P<0.05)。表明CTPP-PEG-PCL胶束临界胶束浓度小,包封率高,肝星状细胞生长抑制效果显著。

To synthetize 3-carboxypropyl-triphenylphosponium bromide-polycaprolacton-CTPP-PEG-PC, and prepare curcumin CTPP-PEG-PCL mieelles 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 MTY assay. The structure of CTPP-PEG-PCL had been identified by IH-NMR spectra. Specifically, the CMC of polymer was 2. 25 mg . L-l , the average size was 190 nm, the drug con- tent was （0. 66±0. 008） g . L -1, and the entrapment efficiency was （94 ±0. 6） %. The in vitro release results showed ettrcumin micelles had a significant higher inhibition ratio in the growth of hepatic stellate cells than crude ettreumin （P 〈 0. 05 ）. This suggested that CTPP-PEG- PCL mieelles feature low CMC, high encapsulation efficiency and notable inhibition effect in growth of hepatic stellate cells.