浸渍离心法制备不同难溶性药物介孔二氧化硅纳米粒载药规律及机制研究

发布时间：2018-08-18 13:01

【摘要】：目的用浸渍离心法制备载不同性质的难溶性药物的介孔二氧化硅纳米粒(MSNs),探寻药物质量浓度与载药量的关系和MSNs载药机制。方法制备空白MSNs,用透射电子显微镜(TEM)和氮气吸附-脱附解析进行表征。以水飞蓟宾、葛根素、盐酸小檗碱、姜黄素和阿魏酸为模型药物,分别固定药物溶液体积和药物质量,采用浸渍离心法载药,测定载药量,分析载药规律,并用紫杉醇、丹参酮IIA和延胡索乙素3种药物对其载药规律进行验证。对载药量较高的水飞蓟宾、葛根素和阿魏酸MSNs进行扫描电子显微镜(SEM)和差示扫描量热法(DSC)表征,分析载药机制。结果空白MSNs粒径为(220±21)nm,比表面积为353.53 m2/g,平均孔径1.53 nm,孔容积率约为0.4 cm3/g。在药载比不变的情况下,无论是固定药物溶液体积,还是固定药物质量,载药量都与药物质量浓度呈线性关系,且与药物性质无关,5种药物的综合回归方程分别为固定药物溶液体积Y=0.351 7 X+0.982 5,r=0.991 4和固定药物质量Y=0.359 2 X+0.248 3,r=0.991 0。SEM显示载药MSNs表面没有明显的药物结晶。载药MSNs的DSC均观察到了药物的熔融峰,但单位吸热量均比等比例的机械混合物明显减小。结论药物溶液质量浓度是决定MSNs浸渍离心法载药效果的关键因素,药物主要以无定形及微晶形式分散于MSNs的介孔中。
[Abstract]:Objective to investigate the relationship between drug concentration and drug loading and the mechanism of MSNs loading in mesoporous silica nanoparticles prepared by impregnation centrifugation. Methods the blank MSNs were prepared and characterized by transmission electron microscopy (TEM) (TEM) and nitrogen adsorption-desorption analysis. Silybin, puerarin, berberine hydrochloride, curcumin and ferulic acid were used as model drugs to immobilize the volume and quality of drug solution respectively. Tanshinone IIA and tetrahydropalmatine were used to verify the drug loading pattern. Silybin, puerarin and ferulic acid MSNs were characterized by scanning electron microscope (SEM) and differential scanning calorimetry (DSC), and the mechanism of drug loading was analyzed. Results the diameter of blank MSNs was (220 卤21) nm, the specific surface area was 353.53 m2 / g, the average pore diameter was 1.53 nm, and the pore volume ratio was about 0.4 cm ~ 3 / g. Under the condition of constant drug loading ratio, whether the volume of the drug solution is fixed or the drug mass is fixed, the drug load is linearly related to the concentration of the drug. Moreover, the comprehensive regression equations of five drugs independent of drug properties were as follows: the volume of fixed drug solution was 0.3517 X 0.982 5U 0.991 4 and the mass of fixed drug was 0.3592 X 0.248 3r0.991 0.SEM. The results showed that there was no obvious drug crystallization on the surface of the drug loaded MSNs. The melting peak of the drug was observed in the DSC loaded with MSNs, but the ratio of absorbed heat to the same proportion of the mechanical mixture was obviously decreased. Conclusion the concentration of drug solution is the key factor to determine the effect of MSNs impregnation centrifugation. The drug is mainly dispersed in the mesoporous of MSNs in amorphous and microcrystalline form.
【作者单位】：西南大学药学院;重庆航天职业技术学院;重庆市江津师范进修学校;
【基金】：西南大学国家级大学生创新创业训练计划项目(201610635023)
【分类号】：R283.6

【参考文献】