Inorganic Drug-Delivery Nanovehicle Conjugated with Cancer-Cell-Specific Ligand
Inorganic Drug-Delivery Nanovehicle Conjugated with Cancer-Cell-Specific Ligand
复制标题
DOI：
10.1002/adfm.200801127
复制
发表时间：
2009-05-22
影响因子：
19
通讯作者：
Choy, Jin-Ho
中科院分区：
文献类型：
--
作者：
Oh, Jae-Min;Choi, Soo-Jin;Choy, Jin-Ho
层状双氢氧化物纳米颗粒是一种潜在的药物递送纳米载体，其表面被癌细胞特异性配体叶酸修饰。通过与氨基丙基三乙氧基硅烷和1-乙基-3-（3-二甲基氨基丙基）-碳二亚胺的逐步偶联反应，成功地完成了表面改性。为了评价叶酸接枝的层状双氢氧化物对癌细胞的靶向作用，采用荧光素5′-异硫氰酸酯标记了含和不含叶酸片段的层状双氢氧化物。利用荧光显微镜观察结合到KB和A549细胞的层状双氢氧化物和叶酸的摄取情况，并用流式细胞术测量。化学和生物实验结果表明，叶酸分子确实与层状双氢氧化物表面结合，因此纳米载体对过表达叶酸受体的癌细胞的选择性增加。本研究表明，层状双氢氧化物纳米颗粒由于与特定配体的化学偶联，可以作为具有靶向功能的药物递送载体。
The surface of layered double hydroxide nanoparticles, a potential drug-delivery nanovehicle, is modified with the cancer-cell-specific ligand, folic acid. The surface modification is successfully accomplished through step-by-step coupling reactions with aminopropyltriethoxysilane and 1-ethyl-3-(3-dimethyl aminopropyl)-carbodiimide. In order to evaluate the cancer-cell targeting effect of folic-acid-grafted layered double hydroxide utilizing fluorescence-related assay, both layered double hydroxide with and without folic acid moiety are labeled with fluorescein 5'-isothiocyanate. The uptake of layered double hydroxide and folic acid conjugated into KB and A549 cells is visualized using fluorescence microscopy and measured by flow cytometry. Both chemical and biological assay results demonstrate that the folic acid molecules are indeed conjugated to the surface of layered double hydroxide and thus the selectivity of nanovehicles to cancer cells overexpressing folate receptors increases. In this study, it is suggested that layered double hydroxide nanoparticles can be used as drug-delivery carriers with a targeting function due to the chemical conjugation with specific ligand.