Nanoemulsion gel-based topical delivery of an antifungal drug: in vitro activity and in vivo evaluation
Nanoemulsion gel-based topical delivery of an antifungal drug: in vitro activity and in vivo evaluation
复制标题
DOI：
10.3109/10717544.2014.933284
复制
发表时间：
2016-02-12
期刊：
影响因子：
6
通讯作者：
Ahmed, F. J.
中科院分区：
文献类型：
--
作者：
Hussain, Afzal;Samad, Abdus;Ahmed, F. J.
目的：在这项研究中，尝试已经集中到制备纳米乳（NE）凝胶局部递送阿替西霉素B（AmB），以增强以及持续的皮肤渗透，在体外抗真菌活性和在体内toxicityassessment.Materials和方法：一系列的NE使用sefsol-218油，吐温80和Transcutol-P通过缓慢自发滴定法制备。制备含有0.1%w/w AmB的卡波姆凝胶（0.5%w/w）。此外，NE凝胶（AmB-NE凝胶）的大小，电荷，pH值，流变学行为，药物释放曲线，皮肤渗透性，溶血性研究和离体大鼠皮肤与大鼠皮肤的相互作用，使用差示扫描量热仪进行了表征。用激光共聚焦显微镜观察药物渗透性，用Draize试验观察皮肤刺激性。采用琼脂扩散法对3株真菌进行了体外抑菌活性研究。在大鼠中进行组织学评估以研究其毒理学潜力。结果和讨论：AmB-NE凝胶（18.090.6 μ g/cm（2）/h）和NE（15.74 +/- 0.4 μ g/cm（2）/h）与药物溶液相比显示出最高的皮肤经皮渗透通量速率（4.59 +/- 0.01 μ g/cm（2）/h），提示更好的替代疼痛和肾毒性静脉给药。溶血和组织病理学结果表明，安全交付的药物。结论：中性粒细胞和AmB-中性粒细胞凝胶是一种有效、稳定、安全的AmB局部给药系统，可用于治疗局部皮肤真菌感染。
Objective: In this study, attempt has been focused to prepare a nanoemulsion (NE) gel for topical delivery of amphotericin B (AmB) for enhanced as well as sustained skin permeation, in vitro antifungal activity and in vivo toxicity assessment.Materials and methods: A series of NE were prepared using sefsol-218 oil, Tween 80 and Transcutol-P by slow spontaneous titration method. Carbopol gel (0.5%w/w) was prepared containing 0.1%w/w AmB. Furthermore, NE gel (AmB-NE gel) was characterized for size, charge, pH, rheological behavior, drug release profile, skin permeability, hemolytic studies and ex vivo rat skin interaction with rat skin using differential scanning calorimeter. The drug permeability and skin irritation ability were examined with confocal laser scanning microscopy and Draize test, respectively. The in vitro antifungal activity was investigated against three fungal strains using the well agar diffusion method. Histopathological assessment was performed in rats to investigate their toxicological potential.Results and discussion: The AmB-NE gel (18.090.6 mu g/cm(2)/h) and NE (15.74 +/- 0.4 mu g/cm(2)/h) demonstrated the highest skin percutaneous permeation flux rate as compared to drug solution (4.59 +/- 0.01 mu g/cm(2)/h) suggesting better alternative to painful and nephrotoxic intravenous administration. Hemolytic and histopathological results revealed safe delivery of the drug. Based on combined results, NE and AmB-NE gel could be considered as an efficient, stable and safe carrier for enhanced and sustained topical delivery for AmB in local skin fungal infection.Conclusion: Topical delivery of AmB is suitable delivery system in NE gel carrier for skin fungal infection.