Gilhotra R M, Mishra D N
Department of Pharmaceutical Sciences, Guru Jambheshwar University of Science and Technology, Haryana, India.
Pharmazie. 2008 Aug;63(8):576-9.
The characteristics of alginate-chitosan films intended for ocular drug delivery of gatifloxacin sesquihydrate were compared with the ionically surface cross-linked films of similar compositions. The effect of polymer ratios and cross-linking was studied relatively to various parameters of formulations including physicochemical, mechanical strength, swelling and bioadhesion. The drug release profiles and drug release mechanisms were compared. The folding endurance, tensile strength, bioadhesive strength considerably increased whereas swelling index, elongation at break decreased with surface cross-linking of the films. Surface cross-linked formulation F3 (2% w/v sodium alginate and 1% w/v chitosan) showed most prolonged drug release of 24 h indicating the potential of surface cross linking of the film to sustain drug release. As per the kinetic models both type of films showed a constant drug release, however the drug release mechanism transformed from erosion to diffusion after cross linking. These results demonstrate that the surface treated alginate-chitosan film could be a potential vehicle to enhance ocular GS bioavailability and patient compliance.
将用于递送加替沙星倍半水合物的藻酸盐-壳聚糖膜的特性与类似组成的离子表面交联膜进行了比较。研究了聚合物比例和交联对制剂各种参数的影响,包括物理化学性质、机械强度、溶胀和生物粘附性。比较了药物释放曲线和药物释放机制。随着膜的表面交联,耐折性、拉伸强度、生物粘附强度显著增加,而溶胀指数、断裂伸长率降低。表面交联制剂F3(2% w/v海藻酸钠和1% w/v壳聚糖)显示出最长24小时的药物释放,表明膜表面交联在维持药物释放方面的潜力。根据动力学模型,两种类型的膜均显示出恒定的药物释放,然而交联后药物释放机制从溶蚀转变为扩散。这些结果表明,表面处理的藻酸盐-壳聚糖膜可能是提高眼部加替沙星生物利用度和患者顺应性的潜在载体。