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基于壳聚糖的口腔膜用于口腔念珠菌病潜在治疗的开发与评价

Development and Evaluation of Buccal Films Based on Chitosan for the Potential Treatment of Oral Candidiasis.

作者信息

Tejada G, Barrera M G, Piccirilli G N, Sortino M, Frattini A, Salomón C J, Lamas María C, Leonardi Darío

机构信息

IQUIR-CONICET, Suipacha 570, 2000, Rosario, Argentina.

Área Técnica Farmacéutica, Departamento Farmacia, Facultad de Ciencias Bioquímicas y Farmacéuticas, Universidad Nacional de Rosario, Suipacha 570, 2000, Rosario, Argentina.

出版信息

AAPS PharmSciTech. 2017 May;18(4):936-946. doi: 10.1208/s12249-017-0720-6. Epub 2017 Jan 20.

Abstract

In this work, chitosan films were prepared by a casting/solvent evaporation methodology using pectin or hydroxypropylmethyl cellulose to form polymeric matrices. Miconazole nitrate, as a model drug, was loaded into such formulations. These polymeric films were characterized in terms of mechanical properties, adhesiveness, and swelling as well as drug release. Besides, the morphology of raw materials and films was investigated by scanning electron microscopy; interactions between polymers were analyzed by infrared spectroscopy and drug crystallinity studied by differential scanning calorimetry and X-ray diffraction. In addition, antifungal activity against cultures of the five most important fungal opportunistic pathogens belonging to Candida genus was investigated. Chitosan:hydroxypropylmethyl cellulose films were found to be the most appropriate formulations in terms of folding endurance, mechanical properties, and adhesiveness. Also, an improvement in the dissolution rate of miconazole nitrate from the films up to 90% compared to the non-loaded drug was observed. The in vitro antifungal activity showed a significant activity of the model drug when it is loaded into chitosan films. These findings suggest that chitosan-based films are a promising approach to deliver miconazole nitrate for the treatment of candidiasis.

摘要

在本研究中,采用流延/溶剂蒸发法,使用果胶或羟丙基甲基纤维素制备壳聚糖膜,以形成聚合物基质。将硝酸咪康唑作为模型药物载入此类制剂中。对这些聚合物膜的机械性能、粘附性、溶胀性以及药物释放进行了表征。此外,通过扫描电子显微镜研究了原材料和膜的形态;通过红外光谱分析聚合物之间的相互作用,并通过差示扫描量热法和X射线衍射研究药物的结晶度。另外,还研究了对属于念珠菌属的五种最重要的真菌性机会致病菌培养物的抗真菌活性。就耐折性、机械性能和粘附性而言,壳聚糖:羟丙基甲基纤维素膜被认为是最合适的制剂。此外,观察到与未载入药物相比,硝酸咪康唑从膜中的溶出率提高了90%。体外抗真菌活性表明,当模型药物载入壳聚糖膜中时具有显著活性。这些发现表明,基于壳聚糖的膜是递送硝酸咪康唑用于治疗念珠菌病的一种有前景的方法。

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