蒙脱石/苦参碱纳米复合物的制备及体外性能的研究

Preparation and in Vitro Properties of Montmorillonite/Matrine Nanocomposite

目的以天然无机纳米矿物蒙脱石作为中药苦参碱的药物载体,以实现对苦参碱的缓释作用。方法首先采用固相研磨法将尿素插入钠基蒙脱石层间以撑大层间距离,再采用溶液共混法将苦参碱药物载入撑大的蒙脱石纳米层间制得蒙脱石/苦参碱复合物;对复合物进行X-射线衍射和红外光谱分析,并进行体外溶出度测试和体外抗肿瘤实验。结果在尿素的协助下苦参碱进入蒙脱石层间,蒙脱石的层间距由1.2 nm增大到1.86 nm;蒙脱石/苦参碱复合物体外数据基本符合Higuchi方程,说明苦参碱的释放量与时间的平方根间呈线性关系,反映出蒙脱石对苦参碱的体外释放具有一定的缓释效果;四甲基偶氮唑蓝实验结果表明,蒙脱石/苦参碱复合物对胃癌细胞(SGC7901)具有显著抑制作用。结论蒙脱石有望成为苦参碱及其他生物碱类药物载体并实现缓释作用,为其在药物制剂领域作为载体材料的研究提供实验依据。

OBJECTIVE To use montmorillonite as the carrier of matrine. METHODS Urea was used to insert into the mont- morillonite interlayer by solid-phase grinding method. After this process, the matrine was loaded by the solution blending to obtain montmorillonite/matrine nanocomposite. RESULTS XRD and FT-IR showed that the urea was intercalated into the montmorillonite layers, and the interlayer spacing of montmorillonite was enlarged from ca. 1.2 to 1.7 nm. With the help of the urea, the matrine was successfully loaded into the montmorillonite layers, at the same time the interlayer distance of the montmorillonite was further increased to 1.86 nm. In vitro release experiments displayed that the release of montmorillonite/matrine composite accorded with the Higuchi e- quation, indicating that the montmorillonite could sustain the release of matrine. MTY measurement showed that the montmorillonite/ matrine nanocomposite has significant cytotoxicity on human gastric cancer cells （ SGC7901 ）. CONCLUSION This research suggests the feasibility of montmorillonite as the sustained release carrier for the matrine and other alkaloids drug, and provides the evidence for montmorillonite in the pharmaceutical field as diug carriers.