Department of Drug Sciences, University of Pavia , Pavia , Italy.
Drug Dev Ind Pharm. 2014 Mar;40(3):352-60. doi: 10.3109/03639045.2012.762654. Epub 2013 Apr 19.
The local treatment of vaginal mucositis requires an intimate and prolonged contact of anti-infective drugs with the mucosa. This can be achieved by means of mucoadhesive and thermally sensitive vehicles, capable of gelifying at the physiological temperature.
The aim of the present work was to compare the potentiality of poloxamer 407 (PLX)/chitosan lactate (CS-L) and CS-L/glycerophosphate (GP) mixtures as mucoadhesive thermally sensitive vehicles for the treatment of vaginal mucositis.
PLX/CS-L and CS-L/GP mixtures were characterized for gelation and mucoadhesion properties as well as for bioactive (antimicrobial and wound healing) properties. Finally, the mixtures were loaded with amoxicillin trihydrate as model drug and characterized for drug release and washability properties.
The addition of CS-L to PLX causes an increase in PLX gelation temperature from 30 °C to the physiological temperature. The dilution with simulated vaginal fluid causes an increase in gelation time of PLX/CS-L mixture, while no variation of such parameter is observed for CS-L/GP mixture which is nevertheless characterized by poorer elastic properties. The stronger mucoadhesion properties of CS-L/GP mixture counterbalance the poorer elasticity of the gel and are responsible for a longer drug contact with the biological substrate. CS-L/GP mixture is moreover characterized by better bioactive properties than PLX-based mixture.
CS-L/GP mixture represents a promising thermally sensitive vehicle.
阴道黏膜炎的局部治疗需要抗感染药物与黏膜进行亲密且长时间的接触。这可以通过具有黏膜附着性和热敏性的载体来实现，这些载体能够在生理温度下胶凝。
本研究旨在比较泊洛沙姆 407（PLX）/乳酸壳聚糖（CS-L）和 CS-L/甘油磷酸（GP）混合物作为治疗阴道黏膜炎的具有黏膜附着性和热敏性的载体的潜力。
对 PLX/CS-L 和 CS-L/GP 混合物的胶凝和黏膜附着特性以及生物活性（抗菌和伤口愈合）特性进行了表征。最后，将混合物加载阿莫西林三水合物作为模型药物，并对其药物释放和可洗性特性进行了表征。
CS-L 的加入使 PLX 的胶凝温度从 30°C升高到生理温度。用模拟阴道液稀释会导致 PLX/CS-L 混合物的胶凝时间增加，而 CS-L/GP 混合物则没有观察到这种参数的变化，尽管 CS-L/GP 混合物的弹性特性较差。CS-L/GP 混合物更强的黏膜附着特性弥补了凝胶较差的弹性，并使药物与生物基质的接触时间更长。CS-L/GP 混合物还具有比基于 PLX 的混合物更好的生物活性特性。
CS-L/GP 混合物是一种很有前途的热敏性载体。
