不同孔径介孔二氧化硅纳米粒的制备及其用于固化西罗莫司自微乳  

Preparation of mesoporous silica nanoparticles in different pore size and its use in the solidification of sirolimus loaded self-microemulsifying drug delivery system

作　　者：余越[1,2] 陶春[1] 杨海跃[1,3] 王天宇[1,3] 薛丹萍 田雪梅[1] 张美敬 房盛楠 宋洪涛[1] 

机构地区：[1]南京军区福州总医院,福建福州350025 [2]福建医科大学药学院,福建福州350108 [3]厦门大学医学院,福建厦门360000

出　　处：《药学学报》2017年第6期985-991,共7页Acta Pharmaceutica Sinica

基　　金：福建省科技计划重点资助项目(2013Y0074)

摘　　要：研究制备了不同孔径的介孔二氧化硅纳米粒及西罗莫司自微乳。使用扫描电镜、透射电镜、小角度X-射线衍射、氮气吸附-脱附表征制得的介孔二氧化硅纳米粒,发现其为有序的纳米孔道结构,孔径分别为6.3、8.1和10.8 nm,通过粒径测定仪测得西罗莫司自微乳粒径为20.6±1.3 nm。通过搅拌法制备载西罗莫司自微乳介孔二氧化硅纳米粒。研究发现,当西罗莫司自微乳与介孔二氧化硅纳米粒质量比2∶1时为最佳比例,载药量约为0.83%,且固体粉末流动性良好。采用差示扫描量热法表明,西罗莫司以非晶体或无定形存在于载体材料中,重分散性良好。孔径大小对于载西罗莫司自微乳介孔二氧化硅纳米粒在250 m L水中2 h的释放终点并没有显著影响,但对于最初40 min释放结果影响较大。综上,介孔二氧化硅纳米粒有望成为一种新型的自微乳吸附剂。The mesoporous silica nanoparticles （MSN） in different pore size and sirolimus （SRL） loaded self-microemulsifying drug delivery system （SMEDDS） were prepared. The results in morphology were collected by scanning electron microscope, transmission electron microscope, small-angle X-ray diffraction, and N2 adsorption-desorption. The results showed that the prepared MSN has ordered nanochannels with a pore size of 6.3, 8.1, 10.8 nm, respectively. The particle size of SRL-SMEDDS were measured by particle sizing system, which was 20.6 ~ 1.3 nm. The stirring method was developed to prepare SRL-SMEDDS-MSN. It was found that the optimal ratio of SRL-SMEDDS to MSN was 2 ： 1, while the drug loading rate was near 0.83%, and the flow properties of SRL-SMEDDS-MSN were of good condition. The differential scanning calorimetry results proving a molecular or amorphous dispersed state of SRL in MSN while the suspension experiment has shown great reconstitution properties of SRL-SMEDDS-MSN. There is no significant influence on maximum drug release rate of different pore size of SRL-SMEDDS-MSN in 250 mL water within 2 h, while the results of the first 40 min have an obvious difference. Above all, MSN might provide a new strategy for the solidification of SMEDDS.

关 键 词：西罗莫司 介孔二氧化硅纳米粒 自微乳化给药系统 固化 纳米载体 体外释放度 

分 类 号：R943[医药卫生—药剂学]