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负载于纳米乳凝胶中的硝酸咪康唑纳米粒的研制,以提高其抗真菌活性。

Development of miconazole nitrate nanoparticles loaded in nanoemulgel to improve its antifungal activity.

作者信息

Tayah Dalal Y, Eid Ahmad M

机构信息

Department of Pharmacy, Faculty of Medicine and Health Sciences, An-Najah National University, Nablus, Palestine.

出版信息

Saudi Pharm J. 2023 Apr;31(4):526-534. doi: 10.1016/j.jsps.2023.02.005. Epub 2023 Feb 22.

Abstract

Miconazole is a synthetic derivative of imidazole, a medication with a broad-spectrum antifungal agent that is used to treat localized vaginal, skin, and nail infections. The aim of the study was to develop an innovative technique to improve the permeability and efficacy of topical miconazole nitrate. A nanoemulgel of miconazole nitrate was formulated by the incorporation of a nanoemulsion and a hydrogel. The nanoemulsion was first optimized using a self-emulsifying technique, and the drug was then loaded into the optimum formulation and evaluated prior to mixing with the hydrogel. Miconazole nitrate nanoemulgel formulations were evaluated for their physical characteristics and antifungal activity. Based on the results, the formulation with 0.4 % Carbopol showed the highest release profile (41.8 mg/ml after 2 h); thus, it was chosen as the optimum formulation. A cell diffusion test was performed to examine the ability of the Miconazole nitrate nanoemulgel to penetrate the skin and reach the bloodstream. Percentage cumulative drug releases of 29.67 % and 23.79 % after 6 h were achieved for the MNZ nanoemulgel and the commercial cream, Daktazol, respectively. The antifungal activity of the novel MNZ nanoemulgel formulation was tested against and compared to Daktazol cream and almond oil; the results were: 40.9 ± 2.3 mm, 25.4 ± 2.7 mm and 18 ± 1.9 mm, respectively. In conclusion, a novel MNZ nanoemulgel showing superior antifungal activity compared to that of the commercial product has been developed. This nanotechnology technique is a step toward making pharmaceutical dosage forms that has a lot of promise.

摘要

咪康唑是咪唑的一种合成衍生物,是一种具有广谱抗真菌作用的药物,用于治疗局部阴道、皮肤和指甲感染。本研究的目的是开发一种创新技术,以提高局部用硝酸咪康唑的渗透性和疗效。通过将纳米乳剂和水凝胶混合制备了硝酸咪康唑纳米乳凝胶。首先采用自乳化技术对纳米乳剂进行优化,然后将药物载入最佳配方中,并在与水凝胶混合之前进行评估。对硝酸咪康唑纳米乳凝胶制剂的物理特性和抗真菌活性进行了评估。根据结果,含0.4%卡波姆的制剂具有最高的释放曲线(2小时后为41.8毫克/毫升);因此,它被选为最佳配方。进行了细胞扩散试验,以检测硝酸咪康唑纳米乳凝胶穿透皮肤并进入血液循环的能力。硝酸咪康唑纳米乳凝胶和市售乳膏达克宁在6小时后的累积药物释放率分别为29.67%和23.79%。对新型硝酸咪康唑纳米乳凝胶制剂的抗真菌活性进行了测试,并与达克宁乳膏和杏仁油进行了比较;结果分别为40.9±2.3毫米、25.4±2.7毫米和18±1.9毫米。总之,已开发出一种新型硝酸咪康唑纳米乳凝胶,其抗真菌活性优于市售产品。这种纳米技术是朝着制备具有很大前景的药物剂型迈出的一步。

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