利用中空羟基磷灰石微球和p H敏感型壳聚糖溶液制备了一种具有良好药物缓释和p H敏感型特性的新型复合药物载体材料。采用组分为19Na2O-17Ca O-64B2O3(wt%)的硼酸盐玻璃在磷酸盐溶液中的原位转化反应制备了多壳层介孔中空HA微球,通过SEM、SEM-EDS、XRD和FTIR等方法对产物微球进行表征。结果表明:微球具有多层介孔中空结构,且属于B型碳酸HA。释药结果表明:中空HA微球在释药初期产生了突释现象,包覆壳聚糖后,复合载体的释药量和释药速率显著下降。与此同时,复合药物载体在不同p H的PBS溶液中表现出p H敏感型药物释放特征,利用浓度20 g/L的壳聚糖溶液包覆的复合载体在p H为6.0、7.4和8.5的PBS溶液中的药物累积释放率分别为85.63%、65.85%和71.85%。
A novel composite drug carrier with excellent sustained and p H-sensitive release performance was prepared by mixing hollow hydroxyapatite(HA) microspheres and chitosan solution with p H-sensitive characteristics. The hollow HA microspheres with mesopores filled on their multilayered spherical shell were obtained by converting borate glass with a novel composition of 19Na2O-17CaO-64B2O3(wt%). The structure, phase composition and morphology of HA microspheres were characterized by SEM, SEM-EDS, XRD, FTIR and N2 adsorption-desorption measurements. The results indicated that the HA microspheres were B-type carbonated HA with hollow structure, in which the carbonate ions occupied the phosphate sites. The drug release results indicated that the HA microspheres generated burst release at initial stage. Coating the hollow HA microspheres with chitosan(CS) reduced the vancomycin release amount and release rate significantly. Meanwhile, the release profile of vancomycin into PBS with different p H value indicated that the CS-coated composite drug carrier shows p H-sensitive release property. The cumulative percentage of vancomycin released into PBS from the CS(20 g/L)-coated composite drug carrier was 85.63%, 65.85% and 71.85% for p H 6.0, 7.4, 8.5, respectively.