文献：

iRGD肽修饰的卡巴他赛白蛋白纳米粒的制备与评价

文献链接：

http://journal11.magtechjournal.com/Jwk_zgyxzz/CN/10.11669/cpj.2023.23.010

作者：

廖蓉惠, 刘喜阳, 李黎, 尹罡, 郑林, 沈雪*, 邓盛齐

相关产品：

磷脂-聚乙二醇-新生Blood vessels 靶向多肽 DSPE-PEG-iRGD

原文摘要：

OBJECTIVE To prepare and optimize cabazitaxel(CTX)-loaded iRGD-modified human serum albumin(HSA) nanoparticles (abbreviated as iRGD-HSA-CTXNPs) and evaluate the drug properties and anti-tumor activity. METHODS HSA-CTX NPs were prepared by ultrasonic homogenization. Box-Behnken design response surface method was used to optimize the prescription. The prepared HSA-CTX NPs were then modified with the cyclic peptide iRGD. The particle size and morphology of the preparation were examined using a laser particle sizer and transmission electron microscope respectively. It was made into a lyophilized powder to improve stability, and the changes in particle size and encapsulation efficiency were examined before and after lyophilization. The in vitro release pattern was investigated using a dialysis method. The in vivo anti-tumor activity was initially investigated by cytotoxicity assay. 

图为：磷脂-聚乙二醇-新生Blood vessels 靶向多肽 DSPE-PEG-iRGD结构式

白蛋白纳米递药体系——以人血白蛋白(human serum albumin,HSA)作为药物载体,通过处方优化制备纳米级粒径且大小均一的环状多肽iRGD修饰的卡巴他赛(cabazitaxel,CTX)白蛋白纳米粒(iRGD-modified cabazitaxel-loaded albumin nanoparticles, iRGD-HSA-CTX NPs)。

方法：采用超声-均质法制备HSA-CTX NPs,响应面Box-Behnken Design筛选,然后利用sulfo-SMCC的交联作用,将环状多肽iRGD修饰到HSA-CTX NPs上,制得iRGD-HSA-CTX NPs。采用激光粒度仪、透射电镜对该制剂的形貌进行考察。为提高稳定性将其制成冻干粉末,并考察冻干前后制剂的粒径及包封率变化。采用透析法考察其体外释放规律。

结果：按优化条件制备的iRGD-HSA-CTX NPs呈球形形貌,分布均匀,平均粒径为(84.37±3.44) nm,多分散系数(polydispersity index,PDI)为(0.237±0.02),Zeta电位为(-4.87±2.09) mV,包封率为(93.67±2.56)%,载药量为(5.13±0.78)%。iRGD-HSA-CTX NPs冻干后制剂稳定性较好,粒径和包封率与冻干前相比未发生明显变化。体外释放结果显示iRGD-HSA-CTX NPs具有一定的缓释效果。超声-均质法和sulfo-SMCC交联作用制备的iRGD-HSA-CTX NPs粒径较小,且粒径分布均匀,药物包封率高。