Dipartamento Farmaco Chimico Tecnologico, Universita'degli Studi di Cagliari, Italy.
Int J Pharm. 2010 Jun 15;392(1-2):92-100. doi: 10.1016/j.ijpharm.2010.03.038. Epub 2010 Mar 23.
The aim of this work was to investigate chitosomes, i.e. liposomes coated by a polyelectrolyte complex between chitosan (CH) and xantan gum (XG), as potential delivery system for oral administration of the protein C-phycocyanin. To this purpose several CH-XG-microcomplexes were prepared in aqueous lactic acid at different chitosan-xanthan gum percent ratios and rheological properties of the microcomplexes were studied to analyse the contribution of chitosan and xanthan gum in the reaction of microcomplexation. After establishing the best microcomplexes, chitosomes were prepared by coating C-phycocyanin loaded liposomes with the CH-XG hydrogels using spray-drying or freeze-drying. The chitosomes were characterized in terms of morphology, size distribution, zeta potential, swelling properties, drug release, and mucoadhesive properties. Rheological studies showed the influence of xanthan gum in the microcomplex properties. Moreover, obtained results demonstrated the effects of formulation and process variables on particle size, drug content, swelling, drug release, and especially on the mucoadhesiveness of C-PC chitosomes of CH-XG. In particular, chitosomes prepared by spray-drying technique using CH-XG in 0.5/8.0 (w/w) ratio showed a regular surface and a drug release characteristic for a Fickian diffusion of the active ingredient. The in vitro mucoadhesive study revealed that the spray-drying method is advantageous to prepare C-phycocyanin loaded chitosomes with excellent mucoadhesive properties for colonic drug delivery.
本工作旨在研究壳聚糖(CH)和黄原胶(XG)之间形成的聚电解质复合物包被的脂质体(chitosomes),即壳聚糖体,作为蛋白质 C-藻蓝蛋白经口给药的潜在传递系统。为此,在不同的壳聚糖-黄原胶比例下,在水性乳酸中制备了几种 CH-XG-微复合物,并研究了微复合物的流变性,以分析壳聚糖和黄原胶在微复合反应中的贡献。在确定最佳微复合物后,使用喷雾干燥或冷冻干燥法,用 CH-XG 水凝胶包被载有 C-藻蓝蛋白的脂质体来制备壳聚糖体。从形态、粒径分布、Zeta 电位、溶胀性能、药物释放和粘膜黏附性能等方面对壳聚糖体进行了表征。流变学研究表明了黄原胶对微复合物性质的影响。此外,研究结果表明,制剂和工艺变量对粒径、药物含量、溶胀、药物释放以及特别是对 CH-XG 的 C-PC 壳聚糖的粘膜黏附性有影响。特别是,使用 CH-XG 为 0.5/8.0(w/w)比例的喷雾干燥技术制备的壳聚糖体具有规则的表面和活性成分呈菲克扩散的药物释放特征。体外粘膜黏附研究表明,喷雾干燥法有利于制备具有优异粘膜黏附性能的载 C-藻蓝蛋白的壳聚糖体,用于结肠药物传递。