壳聚糖修饰甜菜红素脂质体的制备与抗肿瘤活性  

Preparation of Chitosan Coated Liposome Loaded Betanin and Its Antitumor Activity

作　　者：赵振刚[1] 刘爽 游丽君[1] ZHAO Zhengang;LIU Shuang;YOU Lijun(School of Food Science and Engineering,South China University of Technology,Guangzhou 510640,Guangdong,China)

机构地区：[1]华南理工大学食品科学与工程学院,广东广州510640

出　　处：《华南理工大学学报（自然科学版）》2022年第1期16-22,共7页Journal of South China University of Technology(Natural Science Edition)

基　　金：国家自然科学基金资助项目(22078112);新疆生产建设兵团财政科技计划项目(2019AB019,2021BC006)。

摘　　要：甜菜红素是一种水溶性的食品色素,具有多种良好的生物活性,但其稳定性较低,在光照、高pH、高温、酶和氧气存在的情况下容易发生降解,同时甜菜红素的生物利用度较低,不易被人体吸收。本研究制备了壳聚糖修饰的甜菜红素纳米脂质体,以提高甜菜红素的稳定性和生物利用度。采用逆相蒸发法制备甜菜红素纳米脂质体(NLP)。通过测定粒径、电位和多分散指数确定修饰脂质体的最佳壳聚糖浓度,得到壳聚糖修饰的纳米脂质体(CH-NLP),并评价了甜菜红素和两种脂质体对HepG2细胞的抗增殖活性。结果表明NLP的最佳制备条件为:卵磷脂质量浓度60 mg/mL,药脂比1:18,卵胆比6:1,超声处理时间8 min。最佳条件下NLP的包封率为(42.67±1.67)%,载药量为(2.63±0.42)%。壳聚糖与脂质体结合的最佳浓度为0.6%,此时CH-NLP平均粒径为(194.60±4.43)nm,多分散指数(PDI)为(0.29±0.05),Zeta电位为(5.80±0.79)mV。CH-NLP对HepG2细胞的抑制效果最好,NLP次之,其半数效应浓度(EC_(50))分别为(69.46±1.75)和(108.75±2.31)μg/mL;甜菜红素对HepG2细胞的抑制作用最弱。壳聚糖修饰的纳米脂质体作为甜菜红素的载药输送体系,可显著提高甜菜红素的生物活性。Betanin is a water-soluble pigment with lots of biological activities.However,its stability is low and it is easily degraded under light,high pH,high temperature,enzyme and oxygen.Meanwhile,it is of low bioavailability and it's hard to be absorbed by the body.This study aimed to prepare the chitosan coated nanoliposome loaded betanin(CH-NLP)to improve the stability and bioavailability of betanin.Firstly,Nanoliposome loaded betanin(NLP)was prepared by reverse evaporation method.Then average size,Zeta potential and PDI were measured to determine the optimum concentration of CH-NLP.Meanwhile,CH-NLP,NLP and betanin were evaluated for cytotoxicity and antiproliferative activity against HepG2 cells.Results show that the optimum preparation conditions of NLP are as blow:the mass concentration of lectin is 60 mg/mL;the ratio of betanin and lectin is 1:18;the ratio of lectin and cholesterol is 6:1;ultrasound time is 8 min.The encapsulation efficiency of NLP is(42.67±1.67)%,and the drug loading is(2.63±0.42)%.The optimum concentration of chitosan binding to liposomes is 0.6%.The average size,PDI and Zeta potential are(194.60±4.43)nm,(0.29±0.05),(5.80±0.79)mV,respectively.CH-NLP shows the most potent antitumor activity against HepG2 cells,followed by NLP with the EC_(50) of(69.46±1.75)and(108.75±2.31)μg/mL,respectively.Betanin possesses the weakest inhibitory effect against HepG2 cells.Chitosan coated liposome as a novel drug delivery system for betanin can significantly enhance its biological activity.

关 键 词：脂质体 甜菜红素 壳聚糖 抗增殖活性 

分 类 号：TS218[轻工技术与工程—粮食、油脂及植物蛋白工程]