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壳聚糖和一种改性壳聚糖作为改善阴道黏附凝胶性能的试剂。

Chitosan and a modified chitosan as agents to improve performances of mucoadhesive vaginal gels.

作者信息

Perioli Luana, Ambrogi Valeria, Venezia Lorena, Pagano Cinzia, Ricci Maurizio, Rossi Carlo

机构信息

Dipartimento di Chimica e Tecnologia del Farmaco, Università degli Studi di Perugia, Via del Liceo 1, Perugia 06123, Italy.

出版信息

Colloids Surf B Biointerfaces. 2008 Oct 1;66(1):141-5. doi: 10.1016/j.colsurfb.2008.06.005. Epub 2008 Jun 19.

Abstract

New mucoadhesive formulations were designed and studied in order to improve local vaginal therapy by increasing formulation retention prolonging thus drug-mucosa contact time. Some gels were prepared using hydroxyethylcellulose (HEC) alone or mixed with chitosan (CS) or its derivative 5-methyl-pyrrolidinone-chitosan (MPCS) and were loaded with the antibacterial metronidazole (MET) (0.75%). All formulations showed pseudoplastic flow and viscosity increase was observed proportionally to chitosan content (CS>MPCS). Prepared gels showed better extrusion properties (yield stress) than market formulation Zidoval. Mucoadhesion force studies permitted to point out that: (i) CS decreases mucoadhesion force; (ii) MPCS addition increases the mucoadhesion force at high percentage; (iii) all gels containing chitosan showed better mucoadhesive performances than Zidoval. Gels containing MPCS showed higher and faster drug release than those containing CS. All the preparations were able to release higher drug amounts if compared to market formulation. In conclusion MPCS improved gel characteristics in terms of mucoadhesion force, rheological behaviour and drug release pointing out that this modified chitosan is very suitable to obtain manageable and more acceptable vaginal formulation.

摘要

为了通过增加制剂滞留时间从而延长药物与黏膜的接触时间来改善局部阴道治疗,设计并研究了新的黏膜粘附制剂。使用羟乙基纤维素(HEC)单独或与壳聚糖(CS)或其衍生物5-甲基-吡咯烷酮-壳聚糖(MPCS)混合制备了一些凝胶,并负载了抗菌甲硝唑(MET)(0.75%)。所有制剂均表现出假塑性流动,且观察到粘度随壳聚糖含量成比例增加(CS>MPCS)。制备的凝胶比市售制剂Zidoval表现出更好的挤出性能(屈服应力)。黏膜粘附力研究表明:(i)CS降低黏膜粘附力;(ii)高比例添加MPCS可增加黏膜粘附力;(iii)所有含壳聚糖的凝胶比Zidoval表现出更好的黏膜粘附性能。含MPCS的凝胶比含CS的凝胶表现出更高且更快的药物释放。与市售制剂相比,所有制剂都能释放更高剂量的药物。总之,MPCS在黏膜粘附力、流变学行为和药物释放方面改善了凝胶特性,表明这种改性壳聚糖非常适合获得易于管理且更可接受的阴道制剂。

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