Senyiğit Zeynep Ay, Karavana Sinem Yaprak, Eraç Bayri, Gürsel Ozge, Limoncu Mine Hoşgör, Baloğlu Esra
Acta Pharm. 2014 Jun;64(2):139-56. doi: 10.2478/acph-2014-0013.
The aim of the present study was to evaluate chitosan as a vaginal mucoadhesive gel base for econazole nitrate and miconazole nitrate. To this aim, different types of chitosan with different molecular masses and viscosity properties [low molecular mass chitosan (viscosity: 20,000 mPa s), medium molecular mass chitosan (viscosity: 200,000 mPa s), high molecular mass chitosan (viscosity: 800,000 mPa s)] have been used. First, rheological studies were conducted on chitosan gels. Mechanical, syringeability and mucoadhesive properties of chitosan gels were determined. Release profiles of econazole nitrate and miconazole nitrate from chitosan gels were obtained and evaluated kinetically. In addition, anticandidal activities of formulations were determined. Finally, vaginal retention of chitosan gels in rats was evaluated by in vivo distribution studies. Based on the results, it can be concluded that gels prepared with medium molecular mass chitosan might be effectively used for different antifungal agents in the treatment of vaginal candidiosis, since it has high mucoadhesiveness, suitable mechanical and release properties with good vaginal retention.
本研究的目的是评估壳聚糖作为硝酸益康唑和硝酸咪康唑的阴道黏膜黏附凝胶基质。为此，使用了具有不同分子量和黏度特性的不同类型壳聚糖[低分子量壳聚糖（黏度：20,000 mPa·s）、中分子量壳聚糖（黏度：200,000 mPa·s）、高分子量壳聚糖（黏度：800,000 mPa·s）]。首先，对壳聚糖凝胶进行了流变学研究。测定了壳聚糖凝胶的机械性能、可注射性和黏膜黏附性能。获得了硝酸益康唑和硝酸咪康唑从壳聚糖凝胶中的释放曲线并进行了动力学评估。此外，还测定了制剂的抗念珠菌活性。最后，通过体内分布研究评估了壳聚糖凝胶在大鼠体内的阴道滞留情况。基于这些结果，可以得出结论，用中分子量壳聚糖制备的凝胶可能有效地用于治疗阴道念珠菌病的不同抗真菌剂，因为它具有高黏膜黏附性、合适的机械性能和释放性能以及良好的阴道滞留性。
