姜黄素聚乙二醇-聚己内酯纳米粒的药动学及其体外抗肿瘤作用  

Pharmacokinetics and antitumor effect of curcumin loaded polyethylene glycol-polycaprolactone nanoparticles

作　　者：王彬辉[1] 章文红[1] 李范珠[2] 叶晓莉[3] 高晓宇[2] 郭曼曼[2] 戴东波 WANG Binhui;ZHANG Wenhong;LI Fanzhu;YE Xiaoli;GAO Xiaoyu;GUO Manman;DAI Dongbo(Department of Pharmacy,Medical College Affiliated Hospital of Taizhou University,Taizhou 318000,China;College of Pharmaceutical Science,Zhejiang Chinese Medical University,Hangzhou 310000,China;Department of Pharmacy,Hangzhou First Peoples'Hospital,Zhejiang Province,Hangzhou 310006,China;Departmentof Phar-macy,the First Peoples'Hospital of Wenling,Zhejiang Province,Wenling 317500,China)

机构地区：[1]台州学院医学院附属市立医院药剂科,台州318000 [2]浙江中医药大学药学院,杭州310000 [3]浙江省杭州市第一人民医院药剂科,杭州310006 [4]浙江省温岭市第一人民医院药剂科,温岭317500

出　　处：《中国临床药学杂志》2020年第1期1-6,共6页Chinese Journal of Clinical Pharmacy

基　　金：浙江省医药卫生科技计划(编号2011KYB144);浙江省医学会临床科研基金项目(编号2013ZYC-B8);温岭市科技计划项目(编号2016C311090)

摘　　要：目的研究姜黄素聚乙二醇-聚己内酯纳米粒(Cur-PEG-PCL-NPs)在大鼠体内的药动学及其体外抗肿瘤作用。方法采用HPLC法考察Cur-PEG-PCL-NPs在SD大鼠体内的药动学行为;采用MTT法考察Cur-PEG-PCL-NPs体外对人肝癌细胞HepG2的抑制作用。结果姜黄素原药(Cur-Sol)和Cur-PEG-PCL-NPs在大鼠体内的药动学行为均符合二室模型,主要药动学参数分别为:Cur-Sol组t1/2α(7.76±1.80)min,t1/2β(20.11±5.30)min,AUC0→∞(248.59±25.31)mg·min·L^-1,CL(0.08±0.008)mL·min^-1;Cur-PEG-PCL-NPs组t1/2α(4.34±0.66)min,t1/2β(207.20±12.17)min,AUC0→∞(573.06±64.21)mg·min·L^-1,CL(0.04±0.004)mL·min^-1。体外抗肿瘤作用结果表明:Cur-PEG-PCL-NPs较Cur-Sol对HepG2细胞具有更强的抑制作用(P<0.01)。结论制备的Cur-PEG-PCL-NPs具有缓释特性,能延长血中滞留时间,且对HepG2细胞的抑制作用优于Cur-Sol,为后续肝癌治疗提供实验参考。AIM To study the pharmacokinetics of curcumin loaded polyethylene glycol-polycaprolactone nanoparticles(Cur-PEG-PCL-NPs)in rats,and its antitumor effect in vitro.METHODS Pharmacokinetic behav-ior of Cur-PEG-PCL-NPs in SD rats was investigated by HPLC,and MTT assay was used to determine the antitumor activity of Cur-PEG-PCL-NPs on human liver cancer HepG2 cells in vitro.RESULTS Curcumin solution(Cur-Sol)and Cur-PEG-PCL-NPs all fitted into two-compartment model.The pharmacokinetic parameters of Cur-Sol were as follows:t1/2α(7.76±1.80)min,t1/2β(20.11±5.30)min,AUC0→∞(248.59±25.31)mg·min·L^-1 and CL(0.08±0.008)mL·min^-1.The pharmacokinetic parameters of Cur-PEG-PCL-NPs were as follows:t1/2α(4.34±0.66)min,t1/2β(207.20±12.17)min,AUC0→∞(573.06±64.21)mg·min·L^-1 and CL(0.04±0.004)mL·min^-1.Compared with Cur-Sol,Cur-PEG-PCL-NPs can significantly inhibit human HepG2 cells(P<0.01).CONCLUSION Cur-PEG-PCL-NPs show sustained release properties in vivo,and stronger antitu-mor activity in vitro,which could provide experimental reference for the liver cancer treatment。

关 键 词：姜黄素 纳米粒 聚乙二醇-聚己内酯 药动学 抗肿瘤 

分 类 号：R943[医药卫生—药剂学] R965[医药卫生—药学]