【摘要】 为了增加难溶药物的水溶性和结肠靶向性,以吲哚美辛(IDM)为模型药物,采用饱和溶液法制备了IDM/β-环糊精(β-CD)包合物,并以尤特奇S100(ES100)为包衣,用乳化溶剂挥发法制备了IDM/β-CD/ES100纳米粒。通过激光粒度测定仪、扫描电子显微镜、X-射线衍射光谱分析仪和紫外-可见分光光度计对纳米粒进行了分析。结果表明,当IDM/β-CD、ES100比例为1︰1.5时,ES100载IDM/β-CD纳米粒的包封率和载药量分别为57.47%±0.96%和21.14%±0.79%,纳米粒呈球形,分散均匀,平均粒径在260 nm左右,Zeta电位为(-23.0±0.5)mV。体外释药实验显示,当IDM/β-CD、ES100比例为1︰1.5或1︰2时,在pH 1.2的盐酸溶液中,2 h后约有5%的IDM/β-CD释放;再放入pH 6.8的磷酸盐缓冲液(PBS)中,2 h后累积释药量约为27%;最后放入pH 7.8的PBS中,2 h后累积释药量达60%左右,表明该纳米粒具有良好的结肠释药靶向性。更多还原

【Abstract】 To improve the water-solubility and colon-targeting of hydrophobic drugs, theβ-cyclodextrin(β-CD) inclusion complexes and the β-CD/Eudragit S100(ES100) nanoparticles loading with drugs were prepared via saturated water solution method and emulsification solvent evaporation method respectively. Indomethacin(IDM) was selected as a model drug and ES100 was selected as a coating material. The prepared nanoparticles were analyzed by Laser particle size analyzer, Scanning electron microscopy, X-ray diffractometer and Ultraviolet-visible spectrophotometer. The results showed that the nanoparticles were spherical inshape and homogeneously dispersed with average particle sizes of 260 nm and Zeta potential of(-23.0±0.5) mV. When the mass ratio of IDM/β-CD to ES100 was 1 ∶ 1.5, up to 57.47%±0.96% of the encapsulation efficiency and 21.14%±0.79% of the loading capacity were achieved respectively. In vitro release test showed that when the mass ratio of IDM/β-CD to ES100 was 1∶1.5 or 1∶2, about 5% IDM/β-CD was released from the nanoparticles in the pH 1.2 hydrochloric acid solution during the first 2 h. Then transferred the nanoparticles to pH 6.8 phosphate buffer solution(PBS), a cumulative release of 27% was reached after 2 h. Further, when the nanoparticles were transferred to pH 7.8 PBS, acumulative release of 60% was observed after 2 h. This study shows that the nanoparticles have potential to release hydrophobic drugs in the colon.更多还原