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首页> 美国卫生研究院文献>International Journal of Nanomedicine >Development, characterization, and in vivo assessment of mucoadhesive nanoparticles containing fluconazole for the local treatment of oral candidiasis
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Development, characterization, and in vivo assessment of mucoadhesive nanoparticles containing fluconazole for the local treatment of oral candidiasis

机译：含氟康唑的粘膜粘附纳米颗粒在口腔念珠菌病局部治疗中的开发，表征和体内评估

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This study aimed to develop a suitable buccal mucoadhesive nanoparticle (NP) formulation containing fluconazole for the local treatment of oral candidiasis. The suitability of the prepared formulations was assessed by means of particle size (PS), polydispersity index, and zeta potential measurements, morphology analysis, mucoadhesion studies, drug entrapment efficiency (EE), in vitro drug release, and stability studies. Based on the optimum NP formulation, ex vivo drug diffusion and in vitro cytotoxicity studies were performed. Besides, evaluation of the antifungal effect of the optimum formulation was evaluated using agar diffusion method, fungicidal activity-related in vitro release study, and time-dependent fungicidal activity. The effect of the optimum NP formulation on the healing of oral candidiasis was investigated in an animal model, which was employed for the first time in this study. The zeta potential, mucoadhesion, and in vitro drug release studies of various NP formulations revealed that chitosan-coated NP formulation containing EUDRAGIT® RS 2.5% had superior properties than other formulations. Concerning the stability study of the selected formulation, the formulation was found to be stable for 6 months. During the ex vivo drug diffusion study, no drug was found in receptor phase, and this is an indication of local effect. The in vitro antifungal activity studies showed the in vitro efficacy of the NP against Candida albicans for an extended period. Also, the formulation had no cytotoxic effect at the tested concentration. For the in vivo experiments, infected rabbits were successfully treated with local administration of the optimum NP formulation once a day. This study has shown that the mucoadhesive NP formulation containing fluconazole is a promising candidate with once-a-day application for the local treatment of oral candidiasis.
机译：这项研究旨在开发一种合适的含氟康唑的颊黏膜粘附纳米颗粒（NP）制剂，用于局部治疗口腔念珠菌病。通过粒度（PS），多分散指数和ζ电势测量，形态分析，粘膜粘附研究，药物截留效率（EE），体外药物释放和稳定性研究来评估所制备制剂的适用性。基于最佳NP制剂，进行了离体药物扩散和体外细胞毒性研究。此外，使用琼脂扩散法，与杀真菌活性有关的体外释放研究和随时间变化的杀真菌活性对最佳制剂的抗真菌作用进行了评估。在动物模型中研究了最佳NP制剂对口腔念珠菌病愈合的影响，这是本研究中首次使用的动物模型。各种NP制剂的Zeta电位，粘膜粘附和体外药物释放研究表明，含有EUDRAGIT ® RS 2.5％的壳聚糖包衣的NP制剂具有优于其他制剂的性能。关于所选制剂的稳定性研究，发现该制剂稳定6个月。在离体药物扩散研究期间，在受体相中未发现任何药物，这表明有局部作用。体外抗真菌活性研究表明，NP在较长时间内对白色念珠菌的体外功效。同样，该制剂在测试浓度下没有细胞毒性作用。对于体内实验，每天一次局部用最佳NP制剂成功治疗感染的兔子。这项研究表明，含有氟康唑的粘膜粘附性NP制剂是一种有前途的候选药物，每天一次可用于口腔念珠菌病的局部治疗。

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