Wong Tin Wui, Nurjaya Sumiran
Non-Destructive Biomedical and Pharmaceutical Research Centre, Universiti Teknologi MARA, Selangor, Malaysia.
Eur J Pharm Biopharm. 2008 May;69(1):176-88. doi: 10.1016/j.ejpb.2007.09.015. Epub 2007 Oct 1.
The effects of microwave irradiation on the drug release property of pectinate beads loaded internally with chitosan (chitosan-pectinate beads) were investigated against the pectinate beads and beads coacervated with chitosan externally (pectinate-chitosonium beads). These beads were prepared by an extrusion method using sodium diclofenac as the model water-soluble drug. The beads were subjected to microwave irradiation at 80 W for 5, 10, 21 and 40 min. The profiles of drug dissolution, drug content, drug-polymer interaction and polymer-polymer interaction were determined by drug dissolution testing, drug content assay, drug adsorption study, differential scanning calorimetry (DSC) and Fourier transform infra-red spectroscopy (FTIR) techniques. Treatment of pectinate beads by microwave did not lead to a decrease, but an increase in the extent of drug released at 4h of dissolution owing to reduced pectin-pectin interaction via the CO moiety of polymer. In addition, the extent of drug released from the pectinate beads could not be reduced merely through the coacervation of pectinate matrix with chitosan. The reduction in the extent of drug released from the pectinate-chitosonium beads required the treatment of these beads by microwave, following an increase in drug-polymer and polymer-polymer interaction in the matrix. The extent of drug released from the pectinate beads was reduced through incorporating chitosan directly into the interior of pectinate matrix, owing to drug-chitosan adsorption. Nonetheless, the treatment of chitosan-pectinate matrix by microwave brought about an increase in the extent of drug released unlike those of pectinate-chitosonium beads. Apparently, the loading of chitosan into the interior of pectinate matrix could effectively retard the drug release without subjecting the beads to the treatment of microwave. The microwave was merely essential to reduce the release of drug from pectinate beads when the chitosan was introduced to the pectinate matrix by means of coacervation. Under the influences of microwave, the drug release property of beads made of pectin and chitosan was mainly modulated via the CH, OH and NH moieties of polymers and drug, with CH functional group purported to retard while OH and NH moieties purported to enhance the drug released from the matrix.
研究了微波辐照对内部负载壳聚糖的果胶酸盐微球(壳聚糖 - 果胶酸盐微球)药物释放性能的影响,并与果胶酸盐微球和外部与壳聚糖凝聚的微球(果胶酸盐 - 壳聚糖铵微球)进行了对比。这些微球采用挤出法制备,以双氯芬酸钠作为模型水溶性药物。微球在80W功率下分别进行5、10、21和40分钟的微波辐照。通过药物溶出度测试、药物含量测定、药物吸附研究、差示扫描量热法(DSC)和傅里叶变换红外光谱(FTIR)技术来测定药物溶出曲线、药物含量、药物 - 聚合物相互作用和聚合物 - 聚合物相互作用。微波处理果胶酸盐微球在4小时溶出时,由于聚合物的CO基团使果胶 - 果胶相互作用降低,并未导致药物释放程度降低,反而使其增加。此外,仅通过果胶酸盐基质与壳聚糖的凝聚并不能降低果胶酸盐微球的药物释放程度。果胶酸盐 - 壳聚糖铵微球药物释放程度的降低需要对这些微球进行微波处理,这会使基质中药物 - 聚合物和聚合物 - 聚合物相互作用增加。由于药物 - 壳聚糖吸附作用,将壳聚糖直接掺入果胶酸盐基质内部可降低果胶酸盐微球的药物释放程度。然而,与果胶酸盐 - 壳聚糖铵微球不同,微波处理壳聚糖 - 果胶酸盐基质会使药物释放程度增加。显然,将壳聚糖负载到果胶酸盐基质内部可有效延缓药物释放,而无需对微球进行微波处理。当通过凝聚法将壳聚糖引入果胶酸盐基质时,微波对于降低果胶酸盐微球的药物释放才是必不可少的。在微波影响下,由果胶和壳聚糖制成的微球的药物释放性能主要通过聚合物和药物的CH、OH和NH基团进行调节,据推测CH官能团会延缓药物从基质中释放,而OH和NH基团则会促进药物从基质中释放。