Department of Drugs and Pharmaceuticals, School of Pharmaceutical Sciences, São Paulo State University - UNESP, Araraquara, SP, Brazil.
Carbohydr Polym. 2013 Jan 2;91(1):244-52. doi: 10.1016/j.carbpol.2012.08.044. Epub 2012 Aug 20.
In this work pellets containing chitosan for colonic drug delivery were developed. The influence of the polysaccharide in the pellets was evaluated by swelling, drug dissolution and intestinal permeation studies. Drug-loaded pellets containing chitosan as swellable polymer were coated with an inner layer of Kollicoat(®) SR 30 D and an outer layer of the enteric polymer Kollicoat(®) MAE 30 DP in a fluidized-bed apparatus. Metronidazole released from pellets was assessed using Bio-Dis dissolution method. Swelling, drug release and intestinal permeation were dependent on the chitosan and the coating composition. The drug release data fitted well with the Weibull equation, indicating that the drug release was controlled by diffusion, polymer relaxation and erosion occurring simultaneously. The film coating was found to be the main factor controlling the drug release and the chitosan controlling the drug intestinal permeation. Coated pellets containing chitosan show great potential as a system for drug delivery to the colon.
在这项工作中，开发了用于结肠药物传递的壳聚糖微丸。通过溶胀、药物释放和肠道渗透研究评估了多糖对微丸的影响。载药微丸以壳聚糖作为溶胀性聚合物，在流化床设备中用内层 Kollicoat(®) SR 30 D 和外层肠溶聚合物 Kollicoat(®) MAE 30 DP 进行包衣。使用生物分散溶解法评估甲硝唑从微丸中的释放情况。溶胀、药物释放和肠道渗透都依赖于壳聚糖和包衣成分。药物释放数据与 Weibull 方程拟合良好，表明药物释放是由扩散、聚合物松弛和侵蚀同时发生控制的。发现薄膜包衣是控制药物释放的主要因素，壳聚糖控制药物肠道渗透。含有壳聚糖的包衣微丸作为结肠递药系统具有很大的潜力。
