A promising nystatin nanocapsular hydrogel as an antifungal polymeric carrier for the treatment of topical candidiasis
A promising nystatin nanocapsular hydrogel as an antifungal polymeric carrier for the treatment of topical candidiasis
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DOI：
10.1016/j.jddst.2018.12.014
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发表时间：
2019-02-01
影响因子：
5
通讯作者：
Mansy, Soheir S.
中科院分区：
文献类型：
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作者：
AbouSamra, Mona M.;Basha, Mona;Mansy, Soheir S.
本工作的目的是开发和评价制霉菌素（Nys）纳米囊水凝胶，作为一种有吸引力的剂型用于治疗局部念珠菌病。使用纳米沉淀法制备纳米囊分散体。研究了制剂因素，即聚己内酯（PCL）浓度（0.25，0.5%w/w）以及角鲨烯（2.5，5%w/w）和司盘60（Sp 60）（0.5，1%w/w）对所生产制剂的各种物理化学性质的影响。结果揭示了优化的研究因素和纳米囊制剂的显著性;由0.25%w/w PCL、5%w/w角鲨烯和1%w/w Sp 60组成的Nys-NC 6显示出最有利的属性。Nys-NC 6表现出高包封率（86.09 +/-0.28%）、小平均直径（254 +/-6.81nm）、低多分散指数（0.23 +/-3.03）和高负ζ电位（-48 +/-2.00mV）。在掺入卡波姆凝胶后，使用感染的大鼠模型研究Nys-NC 6水凝胶对白色念珠菌的体内抗真菌功效。在治疗期结束时，与Nys水凝胶和市售产品相比，Nys-NC 6水凝胶显示出上级抗真菌效果，真菌计数显著减少，并且根除了尿道感染。所获得的结果进一步得到了共聚焦显微镜和组织病理学显微照片的支持，证实了测试制剂的抗真菌功效。目前的研究结果表明，制霉菌素纳米囊水凝胶是一种成功的治疗局部念珠菌病的方法。
The objective of the present work was the development and evaluation of nystatin (Nys) nanocapsular hydrogel, as an attractive dosage form for treatment of topical candidiasis. The nanocapsular dispersions were prepared using the nanoprecipitation method. The influence of formulation factors, namely, polycaprolactone (PCL) concentration (0.25, o.5% w/w) as well as that of squalene (2.5, 5% w/w) and span 60 (Sp60) (0.5, 1% w/w) was investigated on the various physicochemical properties of the produced formulations. The results revealed the significance of the studied factors which were optimized and the nanocapsular formulation; Nys-NC6 composed of 0.25% w/w PCL, 5% w/w squalene and 1% w/w Sp60 showed the most favorable attributes. Nys-NC6 exhibited high encapsulation efficiency (86.09 +/- 0.28%), small mean diameter (254 +/- 6.81 nm), low poly-dispersity index (0.23 +/- 3.03) and high negative zeta potential (-48 +/- 2.00 mV). After incorporation into Carbopol gel, the in vivo antifungal efficacy of Nys-NC6 hydrogel was studied against Candida albicans using infected rat model. At the end of the treatment period, Nys-NC6 hydrogel showed a superior antifungal effect compared to Nys hydrogel and the market product with a significant reduction of the fungal count and eradication of the Candidal infection. The obtained results were further supported by the confocal microscopy and histopathological photomicrographs confirming the antifungal efficacy of the tested formulation. The current findings suggested that nystatin nanocapsular hydrogel represent a successful approach for the treatment of topical candidiasis.