Department of Pharmaceutics, Global College of Pharmacy , Punjab , India.
Artif Cells Nanomed Biotechnol. 2014 Apr;42(2):95-101. doi: 10.3109/21691401.2013.794351. Epub 2013 May 8.
The occurrence of topical fungal infections is increasing nowadays. Cutaneous fungal infections like cutaneous candidiasis are more prominent in patients associated with AIDS. Current available strategies for the treatment of cutaneous fungal infections are creams or gels which show various adverse effects on skin along with systemic absorption. These drawbacks can be overcome by using various novel drug delivery systems. So, the present investigation aims at exploring the potential of fatty acid vesicles (ufasomes) for the topical delivery of clotrimazole. Oleic acid was employed as a fatty material for the preparation of vesicles. Clotrimazole-loaded oleic acid vesicles were prepared using a thin film hydration method. Prepared vesicles were characterized for size, size distribution, shape, thermal behaviour (differential scanning calorimetry), in vitro release, in vitro antifungal activity, in vitro skin permeation and retention studies and for in vivo antifungal activity. Transmission electron microscopic (TEM) images confirmed the formation of vesicular dispersion (ufasomes) of clotrimazole. Oleic acid vesicles possessed high drug entrapment (49.5 ± 1.0%) and optimum size (455 ± 22 nm) along with good colloidal characteristics (polydispersity index = 0.210 ± 0.035 & zeta potential = - 22.45 ± 0.25 mV) at 4:6 drug-to-oleic acid ratio. In vitro drug release study showed sustained release of drug from the vesicular dispersion. Skin permeation and skin retention studies suggested accumulation of drug in the epidermal part of the skin. In vivo study confirmed prolonged release of drug from oleic acid vesicle up to five days indicating its usefulness for long-term therapy. So, it can be concluded from the present study that fatty acid vesicle may be a good approach to treat topical fungal infections.
如今,局部真菌感染的发生率正在增加。与艾滋病相关的患者更容易出现皮肤真菌感染,如皮肤念珠菌病。目前治疗皮肤真菌感染的策略是使用乳膏或凝胶,这些药物在皮肤和全身吸收方面都有各种不良反应。这些缺点可以通过使用各种新型药物传递系统来克服。因此,本研究旨在探索脂肪酸囊泡(ufa-somes)用于克霉唑局部传递的潜力。油酸被用作制备囊泡的脂肪酸材料。采用薄膜水化法制备载有克霉唑的油酸囊泡。对制备的囊泡进行粒径、粒径分布、形态、热行为(差示扫描量热法)、体外释放、体外抗真菌活性、体外皮肤渗透和保留研究以及体内抗真菌活性进行了评价。透射电子显微镜(TEM)图像证实了囊泡分散体(ufa-somes)的形成。油酸囊泡具有较高的药物包封率(49.5±1.0%)和最佳粒径(455±22nm),以及良好的胶体特性(多分散指数=0.210±0.035和 Zeta 电位=-22.45±0.25mV),在 4:6 的药物-油酸比。体外药物释放研究表明,药物从囊泡分散体中持续释放。皮肤渗透和皮肤滞留研究表明,药物在皮肤的表皮部分积累。体内研究证实,药物从油酸囊泡中释放长达五天,表明其在长期治疗中的有用性。因此,从本研究可以得出结论,脂肪酸囊泡可能是治疗局部真菌感染的一种很好的方法。