Novel super pH-sensitive nanoparticles responsive to tumor extracellular pH
Novel super pH-sensitive nanoparticles responsive to tumor extracellular pH
复制标题
对肿瘤细胞外 pH 值敏感的新型超 pH 敏感纳米颗粒
DOI：
10.1016/j.carbpol.2007.12.006
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发表时间：
2008-08-01
影响因子：
11.2
通讯作者：
Yang, Qian
中科院分区：
文献类型：
--
作者：
Fan, Li;Wu, Hong;Yang, Qian
本研究的目的是评估载有喜树碱（CAMP）的聚（N - 异丙基丙烯酰胺）（NIPAAm）/壳聚糖纳米粒子作为一种对pH敏感的载体，用于特异性靶向肿瘤。通过调节NIPAAm和壳聚糖的质量比，研究了该体系的合成及性质。对纳米粒子的体外药物释放特性进行了研究。结果表明，当NIPAAm与壳聚糖的电荷比达到4 : 1（w/w）时，载药纳米粒子对肿瘤pH最为敏感。包封率和载药量分别为73.7%和8.4%。在37℃下，喜树碱在pH 6.8时的累积释放率最佳，在pH低于6.5或高于6.9时迅速下降。基于MTT（3 -（4,5 - 二甲基噻唑 - 2 - 基）- 2,5 - 二苯基四氮唑）试验和荧光显微镜结果，载喜树碱的纳米粒子在pH 6.8时显示出细胞毒性，而在pH 7.4时细胞毒性极小。对pH敏感的聚NIPAAm/壳聚糖纳米粒子在将抗癌药物递送至靶向组织方面具有一些明显优势。（C）2007爱思唯尔有限公司。保留所有权利。
The objective of this study was to evaluate Camptothecin (CAMP)-loaded poly(N-isopropylacrylamide) (NIPAAm)/chitosan nanoparticles as a pH-sensitive carrier for specifically targeting tumors. The synthesis and properties of the system was studied by adjusting the mass ratio of NIPAAm and chitosan. The drug release characteristics of nanoparticles in vitro were investigated. The results showed that when the charge ratio between NIPAAm and chitosan of 4:1 (w/w) was achieved, the drug-loaded nanoparticles were most sensitive to tumor pH. Encapsulation efficiencies and loading were 73.7% and 8.4%, respectively. The cumulative release rate of CAMP was optimal at pH 6.8 and decreased rapidly either below pH 6.5 or above pH 6.9 in 37 degrees C. Based on MTT (3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium) test and fluorescence microscopy results, CAMP-loaded nanoparticles showed cytotoxicity at pH 6.8 but minimal cytotoxicity at pH 7.4. The pH-sensitive poly NIPAAm/chitosan nanoparticles provided some distinct advantages in delivering anti-cancer drugs to targeted tissues. (C) 2007 Elsevier Ltd. All rights reserved.