多肽修饰雷公藤内酯醇纳米脂质体的制备及抗肿瘤作用  

Preparation of peptide-triptolide nanoliposomes and antitumor studies in vitro

作　　者：阙慧卿 吴彬[2] 李唯 钱丽萍 郭舜民 林绥 QUE Huiqing;WU Bin;LI Wei;QIAN Liping;GUO Shunmin;LIN Sui(Fujian Provincial Key Laboratory of Medical Testing,Institute of Medical Sciences of Fujian Province,Fuzhou,Fujian,350001 P.R.China;Department of Pharmacy,Guangzhou First People's Hospital,Guangzhou,Guangdong,510000 P.R.China)

机构地区：[1]福建省医学科学研究院药物所福建省医学测试重点实验室,福建福州3500012 [2]广州市第一人民医院药学部,广东广州510000

出　　处：《华西药学杂志》2022年第6期608-612,共5页West China Journal of Pharmaceutical Sciences

基　　金：福建省省属公益类科研院所基本科研专项(2018R1031-2)。

摘　　要：目的制备多肽SP94修饰的雷公藤内酯醇纳米脂质体(PTN),并评价其体外抗肿瘤的活性。方法以磷胆比、磷脂与DSPE-PEG-SP94的配比、高压乳匀时间为考察因素,以载药量、包封率、粒径和Zeta电位等综合评分为考察指标,用均匀设计法优选PTN的最佳工艺,并评价PTN的体外抗癌作用。结果PTN最佳制备工艺条件为:大豆卵磷脂:胆固醇:mPEG-DSPE-SP94=10:1:1,高压乳匀10 min。制备得到PTN的载药量为1.078%,载药脂质体对人肝癌细胞HepG2、人前列腺癌细胞PC-3、人乳腺癌细胞MCF-7的半数抑制浓度(IC50)分别为53.91±4.11、117.10±7.35、183.40±11.60 nmol·L^(-1),且在1μmol·L^(-1)时对HepG2、PC-3、MCF-7细胞的增殖抑制率分别为80.53%±0.46%、73.63%±0.37%、77.28%±0.45%。结论通过均匀设计选择的PTN制备方法重复性好,简便可行,制备的PTN对HepG2、PC-3、MCF-7肿瘤细胞具有良好的抑制作用。OBJECTIVE To prepare the polypeptide modified triptolide long cycle nanoemulsion(PTN) and evaluate its antitumor activity in vitro.METHODS In this experiment, the ratio of soybean lecithin to cholesterol, the ratio of soybean lecithin to mPEG-DSPE-SP94 and the high pressure homogenization time were considered as the factors.The drug loading, encapsulation rate, particle size and Zeta potential comprehensive score were used as evaluation indexes.Uniform design method was used to optimize the optimum preparation formula of PTN.MTT assay was conducted to study its anticancer effect on PC-3,HepG2 and MCF-7 cells in vitro.RESULTS The optimal preparation conditions of PTN were as follows: the ratio of soybean lecithin, cholesterol and mPEG-DSPE-SP94 was 10:1:1,with high pressure homogenization for 10 minutes.The drug loading of PTN was 1.078%,and half inhibitory concentration(IC_(50)) on HepG2,PC-3 and MCF-7 was 53.91±4.11 nmol·L^(-1),117.10±7.35 nmol·L^(-1) and 183.40±11.60 nmol·L^(-1),respectively.When the concentration was 1 μmol·L^(-1),PTN inhibited the proliferation of HepG2,PC-3 and MCF-7 cells by 80.53%±0.46%,73.63%±0.37%,and 77.28%±0.45%,respectively.CONCLUSION The PTN preparation method screened through uniform design can be well reproduced, with processing advantages of simple and feasible, and the PTN has a good inhibitory effect on PC-3,HepG2 and MCF-7 cancer cells.

关 键 词：雷公藤内酯醇 DSPE-PEG-SP94 均匀设计 纳米脂质体 HEPG2 PC-3 MCF-7 半数抑制浓度 增值抑制率 

分 类 号：R94[医药卫生—药剂学]