Purpose

The current investigative study was performed to analyze and compare the effect of gellan gum-mixed poloxamer 407 as compared to plain poloxamer 407 on the in situ gelling behavior as well as drug release of the best formulation.

Method

Azelastine hydrochloride-loaded poloxamer 407 micelles and poloxamer 407 gellan gum micelles were prepared with the help of thin film hydration followed by the characterization of the micelles by evaluating the particle size, entrapment efficiency, pH, and gelation as well as in vitro and in vivo drug release analysis.

Result

The azelastine hydrochloride poloxamer 407 with gellan gum micelles having a particle size below 100 nm were found to show low gelation temperature which further increases the retention time of the formulation at the site of administration and results in a controlled release formulation. The in vitro drug release showed significant release of 85% and 89% of drug in the 10^th hour while the in vivo analysis showed similar effect as that of the marketed formulation of Azelast^TM.

Conclusion

A controlled release in situ temperature sensitive gel was successfully formulated which showed significant effect to reduce allergic conjunctivitis.

中文翻译：

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治疗过敏性结膜炎的氮卓斯汀温度敏感原位胶束的配制、开发和比较研究

目的

当前的调查研究旨在分析和比较结冷胶混合泊洛沙姆 407 与普通泊洛沙姆 407 相比对最佳制剂的原位胶凝行为和药物释放的影响。

方法

借助薄膜水化制备了负载氮卓斯汀盐酸的泊洛沙姆 407 胶束和泊洛沙姆 407 结冷胶胶束，然后通过评估粒径、包封效率、pH 和凝胶以及体外和体内表征来表征胶束药物释放分析。

结果

发现具有粒径低于100nm的结冷胶胶束的氮卓斯汀盐酸盐泊洛沙姆407显示出低胶凝温度，这进一步增加了制剂在给药部位的保留时间并产生控释制剂。体外药物释放显示第10小时显着释放85%和89%的药物，^而体内分析显示与Azelast ^TM市售制剂相似的效果。

结论

成功配制出原位控释温敏凝胶，对减轻过敏性结膜炎具有显着效果。