Genta I, Perugini P, Pavanetto F
Department of Pharmaceutical Chemistry, University of Pavia, Italy.
Drug Dev Ind Pharm. 1998 Aug;24(8):779-84. doi: 10.3109/03639049809082726.
Influence of chitosan molecular weight on drug loading and drug release of drug-loaded chitosan microspheres was studied. Chitosans of 70,000 (LC), 750,000 (MC), and 2,000,000 (HC) molecular weight were employed alone or as mixtures (HC/LC 1:1-1:2 w/w). Ketoprofen (ket) was chosen as the model drug to be encapsulated. Microspheres characterized by different theoretical polymer/drug ratios were prepared (2:1, 1:1, 1:2 w/w). Satisfactory ket contents were obtained for all batches of chitosan microspheres with the theoretical polymer/drug ratio 1:2 w/w; microspheres made of HC/LC (1:2 w/w) were characterized by good drug content and encapsulation efficiency independent by polymer/drug ratio. Prepared chitosan microparticulate delivery systems can modulate ket release within 48 hr. Microspheres consisting of HC/LC (1:2 w/w) were the most suitable formulation in controlling drug release.
研究了壳聚糖分子量对载药壳聚糖微球药物负载量和药物释放的影响。使用了分子量分别为70,000(低分子量,LC)、750,000(中等分子量,MC)和2,000,000(高分子量,HC)的壳聚糖,单独使用或作为混合物(HC/LC 1:1 - 1:2重量/重量)。选择酮洛芬(ket)作为待包封的模型药物。制备了具有不同理论聚合物/药物比例(2:1、1:1、1:2重量/重量)的微球。对于所有理论聚合物/药物比例为1:2重量/重量的壳聚糖微球批次,均获得了令人满意的酮含量;由HC/LC(1:2重量/重量)制成的微球具有良好的药物含量和包封效率,且不受聚合物/药物比例的影响。制备的壳聚糖微粒给药系统可在48小时内调节酮的释放。由HC/LC(1:2重量/重量)组成的微球是控制药物释放的最合适制剂。