Laboratoire de Recherche et Développement de Pharmacie Galénique Industrielle, Université de Lyon, Lyon 08, France.
Eur J Pharm Biopharm. 2010 Feb;74(2):255-64. doi: 10.1016/j.ejpb.2009.11.002. Epub 2009 Nov 10.
Conventional formulations of chlorhexidine usually provide short-term efficiency, requiring repeated applications to maintain antibacterial activity. Therefore, appropriate release system of chlorhexidine controlling local drug delivery would reduce the number of applications and enhance patient compliance. The aim of this study was to develop a controlled release system based on medical polyurethane for the local delivery of chlorhexidine diacetate (CDA). CDA-loaded polyurethane films (CDA-Films) and CDA-loaded polyurethane sandwiches (CDA-Sandwiches) were obtained by casting and solvent evaporation. The physico-chemical aspects of CDA-loaded polyurethane systems were investigated, and the crystalline state of CDA in the polymeric system was highlighted. CDA-Films exhibited appropriate mechanical properties for further applications. Drug release was measured in two different media: (i) distilled water and (ii) physiological saline solution to mimic in vivo conditions. Drug release studies were performed up to 11days on CDA-Films and 29days for CDA-Sandwiches. Release of CDA depended on drug loading and the structure of the system. In particular, release of CDA from the sandwich system followed zero-order kinetic. The release rate was significantly lower in physiological solution. Antibacterial studies were carried out on CDA-Films against Staphylococcus aureus and Staphylococcus epidermidis showing 35days persisting antibacterial activity. In conclusion, the polyurethane-based system developed in this study is potentially useful as a local delivery system for CDA and could be used not only in surgery but also in dental and clinical applications.
盐酸氯己定的常规制剂通常提供短期的效率,需要重复应用以保持抗菌活性。因此,适当的盐酸氯己定释放系统控制局部药物输送将减少应用的次数并提高患者的依从性。本研究的目的是开发一种基于医用聚氨酯的局部输送二乙酸盐盐酸氯己定(CDA)的控释系统。通过浇注和溶剂蒸发获得载有 CDA 的聚氨酯薄膜(CDA-Films)和载有 CDA 的聚氨酯三明治(CDA-Sandwiches)。研究了载有 CDA 的聚氨酯系统的物理化学方面,并强调了 CDA 在聚合物系统中的结晶状态。CDA-Films 表现出适合进一步应用的适当机械性能。在两种不同的介质中测量了药物释放:(i)蒸馏水和(ii)生理盐水,以模拟体内条件。对 CDA-Films 进行了长达 11 天的药物释放研究,对 CDA-Sandwiches 进行了长达 29 天的药物释放研究。CDA 的释放取决于药物负载和系统的结构。特别是,夹心系统中 CDA 的释放遵循零级动力学。在生理溶液中的释放速度明显较低。对 CDA-Films 进行了针对金黄色葡萄球菌和表皮葡萄球菌的抗菌研究,显示出长达 35 天的持续抗菌活性。总之,本研究中开发的基于聚氨酯的系统作为 CDA 的局部输送系统具有潜在的用途,不仅可用于手术,还可用于牙科和临床应用。