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Effect on Nail Structure and Transungual Permeability of the Ethanol and Poloxamer Ratio from Cyclodextrin-Soluble Polypseudorotaxanes Based Nail Lacquer

机译:环糊精可溶聚伪轮烷类指甲油对指甲结构和乙醇与泊洛沙姆比率的渗透性的影响

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Aqueous-based nail lacquers have shown potential in promoting the diffusion of drugs into the nail. In our laboratory, we have recently developed a transungual delivery system based on an aqueous dispersion of cyclodextrin-poloxamer soluble polypseudorotaxanes, supramolecular host?guest assemblies that improves the drug permeation into the nail. However, the high-water content and the rheological and adhesive properties of this lacquer negatively affect properties that play a fundamental role in the patients’ acceptance such as stickiness, nail film formation or drying rate, properties. In this work, we have optimized the composition of these lacquers to improve these properties whilst maintaining good drug permeation profiles. Incorporating ethanol into the vehicle and reducing the proportion of Poloxamer 407 (PL), provided a good strategy. The use of hydro-ethanolic mixtures (50% ethanol) and the reduction of the poloxamer concentration significantly improved the lacquer drying speed by reducing the stickiness and promoting film formation on the nail surface. Additionally, in a surprising way, the use of hydro-ethanolic vehicles further enhanced the permeation of ciclopirox olamine and clobetasol propionate, used for the treatment of onychomycosis and nail psoriasis respectively, into the nail and hooves.
机译:水性指甲油已显示出促进药物扩散到指甲中的潜力。在我们的实验室中,我们最近开发了一种基于环糊精-泊洛沙姆可溶性聚假轮烷的水分散液,超分子主客体组件的经耳递送系统,可以改善药物渗透到指甲中的能力。但是,这种清漆的高含水量和流变学和粘合特性会负面影响对患者的接受至关重要的特性,例如粘性,指甲膜形成或干燥速度,特性。在这项工作中,我们优化了这些清漆的成分,以改善这些性能,同时保持良好的药物渗透性。将乙醇掺入车辆中并减少泊洛沙姆407(PL)的比例提供了一个很好的策略。使用水-乙醇混合物(> 50%乙醇)和减少泊洛沙姆的浓度,可通过减少粘性并促进指甲表面的成膜作用来显着提高漆的干燥速度。另外,以令人惊讶的方式,使用水-乙醇媒介物进一步增强了分别用于治疗甲癣和指甲牛皮癣的环吡酮醇胺和丙酸氯倍他索的渗透到指甲和蹄中。

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