Hu Daode, Liu Liang, Chen Wenjuan, Li Sining, Zhao Yaping
Department of Clinical Pharmacology, Shanghai First People's Hospital, Medical College, Shanghai Jiao Tong University, Shanghai 200080, China.
College of Chemistry and Chemical Engineering, Shanghai Jiao Tong University, Shanghai 200240, China.
Int J Mol Sci. 2012;13(5):6454-6468. doi: 10.3390/ijms13056454. Epub 2012 May 24.
In this study, solution enhanced dispersion by supercritical fluids (SEDS) technique was applied for the preparation of 5-aminosalicylic acid (5-ASA) loaded Eudragit S100 (EU S100) nanoparticles. The effects of various process variables including pressure, temperature, 5-ASA concentration and solution flow rate on morphology, particle size, 5-ASA loading and entrapment efficiency of nanoparticles were investigated. Under the appropriate conditions, drug-loaded nanoparticles exhibited a spherical shape and small particle size with narrow particle size distribution. In addition, the nanoparticles prepared were characterized by X-ray diffraction, Differential scanning calorimetry and Fourier transform infrared spectroscopy analyses. The results showed that 5-ASA was imbedded into EU S100 in an amorphous state after SEDS processing and the SEDS process did not induce degradation of 5-ASA.
在本研究中，采用超临界流体增强溶液分散法（SEDS）制备了载有5-氨基水杨酸（5-ASA）的Eudragit S100（EU S100）纳米颗粒。研究了压力、温度、5-ASA浓度和溶液流速等各种工艺变量对纳米颗粒的形态、粒径、5-ASA载药量和包封率的影响。在适当条件下，载药纳米颗粒呈球形，粒径小，粒径分布窄。此外，通过X射线衍射、差示扫描量热法和傅里叶变换红外光谱分析对制备的纳米颗粒进行了表征。结果表明，经SEDS处理后，5-ASA以无定形状态嵌入EU S100中，且SEDS工艺未导致5-ASA降解。
