Self-Assembled Nanospheres of Folate-Decorated Zein for the Targeted Delivery of 10-Hydroxycamptothecin

Self-Assembled Nanospheres of Folate-Decorated Zein for the Targeted Delivery of 10-Hydroxycamptothecin
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用于 10-羟基喜树碱靶向递送的叶酸修饰玉米醇溶蛋白自组装纳米球

DOI:
10.1021/acs.iecr.7b01632
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发表时间:
2017-08-02
影响因子:
4.2
通讯作者:
Jiang, Yanbin
Jiang, Yanbin
中科院分区:
工程技术3区
文献类型:
--
作者:
Liu, Guijin;Pang, Jiafeng;Jiang, Yanbin

文献摘要

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靶向给药是降低药物毒性、提高疗效的有效途径。在本研究中,玉米醇溶蛋白被叶酸(FA)修饰,以实现10-羟基喜树碱(HCPT)的靶向传递。用ATR-UV在线分光光度计监测反应过程,用UV-Vis分光光度计定量测定偶联度。傅立叶变换红外光谱和核磁共振氢谱表明接合成功。详细研究了FA偶联对玉米醇溶蛋白分子自组装和细胞摄取的影响。FA偶联有助于形成具有良好分散性和稳定性的小纳米颗粒,并提高叶酸受体阳性细胞的摄取。制备了羟基喜树碱纳米晶(NC),并将其与FA-Zein复合。羟基喜树碱纳米粒的释药行为比羟基喜树碱纳米粒的骨架溶胀/溶蚀机制更符合扩散机制;羟基喜树碱纳米粒/FA-玉米醇溶蛋白纳米粒具有较高的抗肿瘤活性。
Site-specific drug delivery is an effective approach to decreasing drug toxicity and enhancing therapeutic effects. In this study, zein was decorated with folic acid (FA) for targeted delivery of 10-hydroxycamptothecin (HCPT). The reaction process was monitored using an online ATR-UV spectrophotometer, and the conjugation degree was quantified using a UV–vis spectrophotometer. Successful conjugation was evidenced using FT-IR and 1H NMR. The influence of FA conjugation on the self-assembly of zein molecules and cellular uptake was investigated in detail. FA conjugation facilitates the formation of small nanoparticles with good dispersity and stability and improves the cellular uptake in folate receptor positive cells. HCPT nanocrystals (NC) were prepared and incorporated into FA-zein. The drug release behavior of HCPT NC/FA-zein nanoparticles is more consistent with a diffusion mechanism than a matrix swelling/erosion mechanism of HCPT NC/zein particles; and HCPT NC/FA-zein nanoparticles induce higher anti...