2025-04-11 作者：wff 来源：文献：
Angiopep-2修饰的脑靶向多肽胶束的制备及体外评价
文献链接：
https://mall.cnki.net/magazine/Article/DEJD201804011.htm
作者：
焦秀秀;胡楚玲;何美;丁雪鹰
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原文摘要：
Construct a brain glioma targeted nanomedicine delivery system (LHRss An/DOX) modified with angiopep-2 and loaded with the anti-tumor drug doxorubicin (DOX). Method: LHRss An/DOX peptide micelles loaded with chemotherapy drug DOX were prepared using ultrasonic emulsification method, and the particle size, zeta potential, and appearance morphology of the complex were detected; Measure the drug loading and encapsulation efficiency, and investigate their in vitro release characteristics; The transmembrane transport efficiency of drug loaded micelles was investigated using an in vitro blood-brain barrier (BBB) model, and the intracellular distribution of DOX and its targeting effect on glioma were observed using laser scanning confocal microscopy.
图为：磷脂-聚乙二醇-脑靶向多肽 DSPE-PEG-ANG结构式
该文献构建了angiopep-2修饰的硫辛酸-聚精氨酸组氨酸(LHRss)多肽纳米胶束并包载多柔比星(DOX)的靶向纳米给药系统(LHRss-An/DOX)。
具体制备方法：采用超声乳化法制备包载DOX的多肽胶束LHRss-An/DOX,检测复合物的粒径、zeta电位和外观形态;测定载药量和包封率,并对其体外释放特性进行考察;通过体外BBB模型考察载药胶束的跨膜转运效率,使用激光扫描共聚焦显微镜观察DOX胞内的分布情况及的靶向性。
结果：胶束LHRss-An/DOX呈球形,平均粒径为(100.9±8.7)nm,聚合物分散性指数为0.232,电位为(28.8±3.3)m V,药载比为40%,载药量为15.8%,包封率为55.3%,在pH 7.4、pH 5.5和pH 5.5+10 mmol/L DL-二硫苏糖醇(DTT)环境下72 h内的累积释放率分别为(60.3±2.6)%、(84.1±3.9)%和(96.6±2.7)%;LHRss-An/DOX的跨BBB效率分别是LHRss/DOX和游离DOX的2.04和4.27倍,差异有统计学意义(P<0.05);经过angiopep-2修饰的载药纳米胶束的跨BBB能力及的靶向性增强,是一种潜在的靶向给药系统。
