Cho Sang-Min, Choi Hoo-Kyun
College of Pharmacy, Chosun University, Gwangju 501-759, Korea.
Arch Pharm Res. 2005 May;28(5):612-8. doi: 10.1007/BF02977767.
A mucoadhesive microsphere was prepared by an interpolymer complexation and solvent evaporation method, using chitosan and poly(acrylic acid) (PAA), to prolong the gastric residence time of the delivery system. The Fourier transform infrared results showed that microspheres were formed by an electrostatic interaction between the carboxyl groups of the PAA and the amine groups of the chitosan. X-ray diffraction and differential scanning calorimetry analysis showed that the enrofloxacin in the chitosan-PAA microsphere was molecularly dispersed in an amorphous state. Scanning electron microscopy of the surface and the quantity of mucin attached to the microspheres indicated that chitosan-PAA microspheres had a higher affinity for mucin than those of chitosan alone. The swelling and dissolution of the chitosan-PAA microspheres were found to be dependent on the pH of the medium. The rate of enrofloxacin released from the chitosan-PAA microspheres was slower at higher pH; therefore, based on their mucoadhesive properties and morphology, the chitosan-PAA microspheres can be used as a mucoadhesive oral drug delivery system.
采用聚合物络合和溶剂蒸发法,以壳聚糖和聚丙烯酸(PAA)制备了一种粘膜粘附微球,以延长给药系统在胃中的停留时间。傅里叶变换红外光谱结果表明,微球是由PAA的羧基与壳聚糖的胺基之间的静电相互作用形成的。X射线衍射和差示扫描量热分析表明,壳聚糖-PAA微球中的恩诺沙星以分子形式分散于无定形状态。微球表面的扫描电子显微镜观察及附着于微球的粘蛋白数量表明,壳聚糖-PAA微球对粘蛋白的亲和力高于单独的壳聚糖微球。发现壳聚糖-PAA微球的溶胀和溶解取决于介质的pH值。壳聚糖-PAA微球中恩诺沙星在较高pH值下的释放速率较慢;因此,基于其粘膜粘附特性和形态,壳聚糖-PAA微球可作为一种粘膜粘附口服给药系统。