三维有序大孔二氧化硅作为药物载体的制备及体外释药特性

Preparation of 3-D ordered macroporous silica as drug carrier and release characteristics in vitro

目的:制备三维有序大孔(three-dimensional ordered macroporous,3DOM)二氧化硅作为难溶性药物尼群地平的载体,对三维有序大孔结构进行表征,考察其体外释药特性。方法:采用聚甲基丙烯酸甲酯(PMMA)胶体晶体模板法制备3DOM二氧化硅载体,通过溶剂沉积法将药物载入载体中。采用场发射扫描电子显微镜(SEM)进行孔结构的表征,粉末X射线衍射法(XRD)考察药物在载体中的存在状态,傅里叶变换红外(FT-IR)光谱法研究药物与载体的相互作用,考察载药量对体外释药的影响。结果:PMMA胶体晶体模板法制得的3DOM二氧化硅载体呈三维有序多孔网状结构,当药物-载体质量比为1∶3和1∶5时,药物的结晶状态明显减弱,在2 h时体外释放度达到80%。结论:PMMA胶体晶体模板法成功制备了3DOM二氧化硅,作为难溶性药物载体能显著提高其体外溶出性。

Objective:To prepare and characterize 3D ordered macroporous (3DOM)silica as drug car-rier for poorly water soluble drugs and investigate its in vitro release characteristics.Methods:3DOMsilica carrier was prepared using PMMA colloidal crystal template method and drug was incorporated into pores of 3DOMsilica matrix through a solvent deposition procedure.The pore structure was characterized was stud-ied by scanning electron microscopy (SEM).The solid state of drug in 3DOMsilica was evaluated by X-ray diffraction (XRD).Inter-molecular interaction of drug and matrix was obtained using a FT-IR spectrome-ter.The release property in vitro was investigated.Results:Silica carrier obtained showed exactly a three-dimensional ordered macroporous structure.There was a significant loss of the drug crystallinity at drug-car-rier ratio of 1 ∶3 and 1 ∶5,and the release rate in vitro reached 80% in 2 hours.Conclusion:3DOMsili-ca was successfully prepared using colloidal crystal template method,and the dissolution of poorly water sol-uble drug was improved significantly.