Segale Lorena, Giovannelli Lorella, Mannina Paolo, Pattarino Franco
Dipartimento di Scienze del Farmaco, Università del Piemonte Orientale, Largo Donegani 2, 28100 Novara, Italy.
Scientifica (Cairo). 2016;2016:5062706. doi: 10.1155/2016/5062706. Epub 2016 Apr 3.
In this work alginate and alginate-chitosan beads containing celecoxib solubilized into a self-emulsifying phase were developed in order to obtain a drug delivery system for oral administration, able to delay the drug release in acidic environment and to promote it in the intestinal compartment. The rationale of this work was linked to the desire to improve celecoxib therapeutic effectiveness reducing its gastric adverse effects and to favor its use in the prophylaxis of colon cancer and as adjuvant in the therapy of familial polyposis. The systems were prepared by ionotropic gelation using needles with different diameters (400 and 600 μm). Morphology, particle size, swelling behavior, and in vitro drug release performance of the beads in aqueous media with different pH were investigated. The experimental results demonstrated that the presence of chitosan in the formulation caused an increase of the mechanical resistance of the bead structure and, as a consequence, a limitation of the bead swelling ability and a decrease of the drug release rate at neutral pH. Alginate-chitosan beads could be a good tool to guarantee a celecoxib colon delivery.
在这项工作中,开发了含有溶解在自乳化相中塞来昔布的海藻酸盐和海藻酸盐-壳聚糖珠,以获得一种口服给药的药物递送系统,该系统能够在酸性环境中延迟药物释放,并在肠道中促进药物释放。这项工作的基本原理与提高塞来昔布治疗效果、减少其胃部不良反应以及有利于其用于结肠癌预防和家族性息肉病治疗辅助的愿望有关。通过使用不同直径(400和600μm)的针头进行离子凝胶化制备这些系统。研究了珠子在不同pH值的水性介质中的形态、粒径、溶胀行为和体外药物释放性能。实验结果表明,制剂中壳聚糖的存在导致珠子结构的机械抗性增加,结果是珠子溶胀能力受限,并且在中性pH下药物释放速率降低。海藻酸盐-壳聚糖珠可能是保证塞来昔布结肠递送的良好工具。