载穿心莲内酯的氨基修饰介孔二氧化硅纳米粒的制备及其初步药效学评价

Preparation and Preliminary Pharmacodynamic Evaluation of Amino-modified Mesoporous Silica Nanoparticles Loaded with Andrographolide

采用3种方法制备了氨基修饰的介孔二氧化硅纳米粒(NH2-MSN),对其形貌和结构进行表征。选用其中1种具有较大的比表面积(1 227.4 m2/g)和孔容积(0.67 m3/g)、介孔形状规则且孔径均一的NH2-MSN(称为M3)。该制品的平均粒径为(148.1±3.1)nm,?电位为(37.04±0.22)m V。用其与穿心莲内酯照1∶1的质量比投料制备纳米粒,结果载药量及包封率为(41.7±2.3)%和(80.7±4.7)%。建立了二甲苯致小鼠耳肿胀模型,初步评价该载药纳米粒的药效。结果表明,与穿心莲内酯混悬液及市售片剂相比,该载药纳米粒的抗炎作用较优。

The amino-modified mesoporous silica nanoparticles （NH2-MSN） were prepared by three methods, and their morphologies and structures were characterized. One of the prepared NH2-MSN, named as M3, with large specific surface area of 1 227.4 m^2/g, pore volume of 0.67 m^3/g, uniform size and oriented well-defined mesopores was selected. The average particle size and ζ potential of M3 were （148.1±3.1）nm and （37.04±0.22）mV. The drug loading and entrapment efficiency of andrographolide in the product prepared with M3 and andrographolide in the feed ratio of 1 ： 1 were （41.7±2.3） % and （80.7±4.7） %. The pharmacodynamics of the product was preliminary investigated with the xylene-induced mouse ear edema model. The results showed that the anti-inflammatory effect of the product was superior to those of andrographolide suspensions and commercially available tablets.