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以聚乳酸–羟基乙酸共聚物(PLGA)和纳米羟基磷灰石(nHA)作为生物降解材料制备了药物替莫唑胺(Temozolomide,TMZ)的缓释系统。采用湿法化学工艺制备了球状和棒状的nHA粉末。将TMZ药物分子负载在nHA表面(nHA-TMZ),再通过乳化溶剂挥发法将nHA-TMZ包裹在PLGA微球中,同时研究了微球中nHA的形貌和含量对缓释微球物化性能的影响。用扫描电镜、紫外分光光度计分别测定了微球的结构、形貌、药物包封率和缓释行为。相比于不含有nHA的TMZ/PLGA缓释微球,nHA的介入能够显著提高药物的包封率,并且包封率与nHA的加入量有关。此外,药物释放实验表明包裹在微球中的nHA的形貌和溶解速率能够影响微球的缓释行为。
The sustained-release system of Temozolomide (TMZ) was prepared with polylactic-co-glycolic acid (PLGA) and nano-hydroxyapatite (nHA) as biodegradable materials. Spherical and rod-shaped nHA powders were prepared by a wet chemical process. TMZ drug molecules were loaded on the nHA surface (nHA-TMZ), and then nHA-TMZ was encapsulated in the PLGA microspheres by the emulsion solvent evaporation method. Meanwhile, the morphology and content of nHA in the microspheres were investigated. Impact. The structure, morphology, drug entrapment efficiency and sustained release behavior of the microspheres were determined by scanning electron microscopy and ultraviolet spectrophotometer. Compared with TMZ / PLGA sustained release microspheres without nHA, nHA intervention significantly increased the encapsulation efficiency of the drug, and the entrapment efficiency was related to the addition of nHA. In addition, drug release experiments showed that the morphology and dissolution rate of nHA encapsulated in microspheres can affect the sustained-release behavior of microspheres.