pH-Sensitive Podophyllotoxin Carrier for Cancer Cells Specific Delivery
pH-Sensitive Podophyllotoxin Carrier for Cancer Cells Specific Delivery
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DOI：
10.1002/pc.20765
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发表时间：
2010-01-01
影响因子：
5.2
通讯作者：
Yang, Tie-hong
中科院分区：
文献类型：
--
作者：
Fan, Li;Wu, Hong;Yang, Tie-hong
基于N-异丙基丙烯酰胺（NIPAAm）和壳聚糖缀合物，建立了针对实体瘤的pH敏感药物靶向系统。调整NIPAAm和壳聚糖的质量比以获得超pH敏感特性，并利用傅里叶变换红外光谱仪研究其结构，证实纳米粒子的成功合成。还研究了pH敏感性和体外药物释放特性。使用人肺癌细胞A-549和人成纤维细胞测试空白和鬼臼毒素（POD）负载纳米粒子的生物相容性，进一步证明靶向酸性肿瘤细胞外pH的可靠性。结果表明，当NIPAAm和CS之间的电荷比达到4:1(w/w)时，直径范围为50至150 nm的载药纳米粒子对肿瘤pH表现出超pH敏感响应。封装和装载效率分别为63.7%和2.4%。 POD 的累积释放速率在 pH 6.8 时显着增强，而在 pH 6.5 以下或 pH 6.9 以上（37 ℃）时迅速下降。在 pH 6.8 时，负载 POD 的纳米粒子在 MTT 测试和荧光显微镜研究中显示出细胞毒性，与相同 POD 浓度下的游离 POD 相当，而在 pH 7.4 时，在测试浓度范围内几乎没有细胞毒性。因此，无毒的PNIPAAm-g-壳聚糖纳米粒子具有作为新型抗癌药物载体的潜力。聚合物。 COMPOS., 31:51-59, 2010。(C) 2009 年塑料工程师协会
A pH-sensitive drug targeting system for solid tumors was established based on N-isopropylacrylamide (NIPAAm) and chitosan conjugates. The mass ratio of NIPAAm and chitosan was adjusted to obtain super pH-sensitive characteristic and the structure was studied by using Fourier transform infrared spectroscope to confirm the successful synthesis of the nanoparticles. The pH-sensitive and drug release characteristics in vitro were studied as well. Human lung cancer cells A-549 and human fibroblast were used to test the biocompatibility of blank and Podophyllotoxin (POD) loaded nanoparticles further to certificate the reliability of targeting acidic tumor extracellular pH. Results revealed that when charge ratio between NIPAAm and CS achieve 4:1(w/w), the drug-loaded nanoparticles, which diameters ranged from 50 to 150 nm, exhibited super pH-sensitive responses to tumor pH. Encapsulation and loading efficiencies were 63.7% and 2.4%, respectively. The cumulative release rate of POD, which significantly enhanced at pH 6.8 while decreased rapidly either below pH 6.5 or above pH 6.9 at 37 degrees C. At pH 6.8, POD-loaded nanoparticles showed cytotoxicity in MTT test and fluorescence microscopic study, comparable to that of free POD at the same POD concentrations, whereas at pH 7.4 there was little cytotoxicity at the tested concentration range. Thereby, the atoxic PNIPAAm-g-chitosan nanoparticle has the potentiality as a novel anticancer drugs carrier. POLYM. COMPOS., 31:51-59, 2010. (C) 2009 Society of Plastics Engineers