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,YMZ)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nI--IA—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F/HA的形貌和溶解速率能够影响微球的缓释行为。
The temozolomide (TMZ) controlled release system with poly (d-l-lactic-co-glycolic acid) (PLGA) biodegradable polymer and nano-hydroxyapatite particles (nHA) was investigated. The nHA crystals with a rod-like or spherical morphology were prepared by a wet chemical process. The TMZ loaded nHA particles were encapsulated in the PLGA microspheres (abbreviated nHA-TMZ/ PLGA) by a solid/oil/water (S/O/W) technique. Meanwhile, the influences of nHA morphology as well as the nHA amount in the preparation on release properties of microspheres were investigated. The microspheres structure, the morphology, the drug encapsulation efficiency and its release process were characterized by scanning electron microscopy and ultra-violet spectrometry, respectively. The results demonstrate that compared to the TMZ/PLGA microspheres, the introduction of nHA component can enhance the efficiency of drug encapsulation due to the quantity increase of the nHA-TMZ during fabrication. Furthermore, it was indicated that the morphology and dissolution of the nHA incorporated in the microspheres both had an impact on the TMZ release behavior.