氨基表面修饰有序介孔硅对槲皮素的载药性能及药物释放影响研究

 目的 制备氨基修饰有序介孔硅(amino-modified ordered mesoporous silica, NH₂-OMS)并考察其作为水难溶性药物载体的载药及体外释放性能。方法 以十六烷基三甲基溴化铵为模板合成了有序介孔硅(OMS),并以3-氨丙基三甲氧基硅烷对其表面进行修饰,以槲皮素为模型药物,并利用N₂ 吸附-脱附、X-射线衍射、热重分析等方法对载药前后的氨基修饰有序介孔硅进行表征。考察氨基修饰有序介孔硅的载药性能及药物的体外释放行为。结果 当槲皮素浓度为4 mmol·L^-1、载药24 h、50 ℃时,氨基修饰有序介孔硅对槲皮素的载药量为21.0%,包封率为58.2%。槲皮素氨基修饰有序介孔硅药粒在模拟肠液和模拟胃液中的药物释放量分别是槲皮素原料药溶解量的13和27倍。 结论 氨基修饰有序介孔硅作为水难溶性药物槲皮素的载体可以明显改善其水溶性及在胃肠道中的溶出度。

Inclusion of Quercetin in Amino-group Modified Ordered Mesoporous Silica:Drug Loading and Release Properties

OBJECTIVE To prepare amino-modified ordered mesoporous silica (NH₂-OMS) as a drug carrier and test the loading and release properties of poorly water soluble drug carried by it. METHODS OMS was first prepared using cetyltrimethyl ammonium bromide as the template and then modified by 3-aminopropyl trimethoxy silane to prepare NH₂-OMS. N₂ adsorption-desorption, X-ray diffraction and thermogravimetric analysis were used to characterize the NH₂-OMS. Quercetin was loaded onto NH₂-OMS in order to explore the drug loading properties of NH₂-OMS. RESULTS The drug loading and entrapment efficiency of quercetin-NH₂-OMS were about 21.0% and 58.2%, respectively, when the concentration of quercetin was 4 mmol·L^-1, the reaction time was 24 h and the temperature was set at 50 ℃. The in vitro release test demonstrated that quercetin-NH₂-OMS could form supersaturated solution in simulated intestinal fluid and gastric fluid at concentrations of 13-fold and 27-fold of the thermodynamic solubility of quercetion. CONCLUSION NH₂-OMS, as the carrier for quercetin, can significantly increase its water solubility and release rate in intestinal and gastric fluids.