IQUIR-CONICET, Suipacha 570, 2000 Rosario, Argentina.
IQUIR-CONICET, Suipacha 570, 2000 Rosario, Argentina; Área Bromatología y Nutrición, Departamento de Ciencias de los Alimentos y del Medio Ambiente, Facultad de Ciencias Bioquímicas y Farmacéuticas, Universidad Nacional de Rosario, Suipacha 570, 2000 Rosario, Argentina.
Mater Sci Eng C Mater Biol Appl. 2017 Oct 1;79:140-150. doi: 10.1016/j.msec.2017.05.034. Epub 2017 May 8.
Oral candidiasis is the most common opportunistic infection affecting patients with the human immunodeficiency virus. Miconazole buccal tablets or miconazole gel are approved for the treatment of oropharyngeal candidiasis. However, buccal films present more flexibility and also offer protection for the wounded mucosa, reducing pain. Due to their small size and thickness, buccal films may improve patients' compliance, compared to tablets. Additionally, they may increase the relatively short residence time on the mucosa of oral gels, which are easily removed by saliva. Polymeric films loaded with miconazole nitrate were prepared by a casting/solvent evaporation methodology using chitosan, carbopol, gelatin, gum arabic, and alginate to form the polymeric matrices. The morphology of films was investigated by scanning electron microscopy; interactions between polymers were analyzed by infrared spectroscopy and drug crystallinity by differential thermal analysis and X-ray diffraction. Films were characterized in terms of thickness, folding endurance, tensile properties, swelling, adhesiveness, and drug release. Finally, the antifungal activity against cultures of the five most important fungal opportunistic pathogens belonging to Candida genus was investigated. The more appropriate formulations were those based on chitosan-gelatin and chitosan-carbopol which showed good mechanical properties and adhesiveness, a relative low swelling index, improved drug release, and showed better in vitro activity against Candida cultures than miconazole nitrate raw material. Thus, it will be possible to produce a new pharmaceutical form based on polymeric films containing chitosan and miconazole nitrate, which could be loaded with low drug concentration producing the same therapeutic effect against Candida cultures.
口腔念珠菌病是影响人类免疫缺陷病毒患者的最常见机会性感染。咪康唑口腔贴片或咪康唑凝胶已被批准用于治疗口咽念珠菌病。然而，口腔膜具有更大的灵活性，并且还可以为受伤的粘膜提供保护，减轻疼痛。由于其体积小且厚度薄，与片剂相比，口腔膜可能会提高患者的依从性。此外，它们可能会增加口腔凝胶在粘膜上相对较短的停留时间，因为口腔凝胶很容易被唾液清除。通过使用壳聚糖、卡波姆、明胶、阿拉伯胶和海藻酸钠形成聚合物基质，采用浇铸/溶剂蒸发方法制备负载硝酸咪康唑的聚合物膜。通过扫描电子显微镜研究了薄膜的形态；通过红外光谱分析了聚合物之间的相互作用，通过差示热分析和 X 射线衍射分析了药物结晶度。从厚度、耐折性、拉伸性能、溶胀性、粘附性和药物释放等方面对薄膜进行了表征。最后，研究了对抗五种最重要的真菌机会性病原体（属于念珠菌属）的培养物的抗真菌活性。更合适的配方是基于壳聚糖-明胶和壳聚糖-卡波姆的配方，它们具有良好的机械性能和粘附性、相对较低的溶胀指数、改善的药物释放，并显示出比硝酸咪康唑原料药更好的体外抗念珠菌活性。因此，有可能基于含有壳聚糖和硝酸咪康唑的聚合物膜生产一种新的药物制剂，该制剂可以装载低药物浓度，对念珠菌培养物产生相同的治疗效果。
