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Y-shaped methoxy poly (ethylene glycol)-block-poly (epsilon-caprolactone)-based micelles for skin delivery of ketoconazole: in vitro study and in vivo evaluation

机译:Y型甲氧基聚(乙二醇)嵌段聚(ε-己内酯)基胶束用于酮康唑的皮肤递送:体外研究和体内评价

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摘要

Ketoconazole is a hydrophobic broad-spectrum antifungal agent for skin infection therapy. In order to develop topical formulation of ketoconazole for improving its selective skin deposition and water-solubility, ketoconazole-loaded Y-shaped monomethoxy poly(ethylene glycol)-block-poly(ε-caprolactone) micelles were prepared through thin-film hydration method with high entrapment efficiency (96.1 ± 0.76%) and small particle (about 58.66 nm). The drug-loaded micelles showed comparative in vitro antimicrobial activity with KET cream. In ex in vivo skin deposition and permeation study, ketoconazole-loaded micelles provided skin accumulation higher than marketed ketoconazole cream without obvious permeation in the whole period. Fluorescence microscopy study and histopathological study demonstrated the copolymeric micelles' penetrating into skin in depth due to its capability of weakening the barrier function of stratum corneum. In vivo skin deposition parameters further confirmed high skin deposition of drug-loaded micelles (AUC_((0-t)) = 396.16 μg·h/cm~2) over marketed ketoconazole cream (AUC_((0-t)) = 250.03 μg·h/cm~2). Meanwhile, in vivo pharmacokinetic parameters proved that ketoconazole-loaded micelles reduced ketoconazole's distribution in blood in comparison with the cream (AUC_((0-t)) = 93,028.00 μg·h/L vs AUC_((0-t)) = 151,714.00 μg·h/L), meaning lower possibility of its systemic unwanted effects in the skin fungal infection treatment. The results suggested that the copolymeric micelles can be adopted for specific delivering ketoconazole into skin for fungal infection cure.
机译:酮康唑是用于皮肤感染治疗的疏水性广谱抗真菌剂。为了开发酮康唑的局部制剂以改善其选择性皮肤沉积和水溶性,通过薄膜水化法制备了酮康唑负载的Y型Y型单甲氧基聚(乙二醇)-嵌段-聚(ε-己内酯)胶束。高包封率(96.1±0.76%)和小颗粒(约58.66 nm)。载有药物的胶束与KET乳霜相比具有体外抗微生物活性。在离体皮肤沉积和渗透性研究中,负载酮康唑的胶束提供的皮肤蓄积量高于市售的酮康唑乳膏,且整个时期内均无明显渗透。荧光显微镜研究和组织病理学研究表明,共聚胶束由于其削弱角质层屏障功能的能力而深入皮肤。体内皮肤沉积参数进一步证实了载药胶束(AUC _((0-t))= 396.16μg·h / cm〜2)较市售酮康唑乳膏(AUC _(((0-t))= 250.03μg)的皮肤沉积量高·h / cm〜2)。同时,体内药代动力学参数证明与乳膏相比,酮康唑负载的胶束减少了酮康唑在血液中的分布(AUC _((0-t))= 93,028.00μg·h / L vs AUC _((0-t))= 151,714.00μg ·h / L),这意味着在皮肤真菌感染治疗中出现全身性不良作用的可能性较低。结果表明,可采用共聚胶束将酮康唑特异递送至皮肤,以治愈真菌感染。

著录项

  • 来源
    《Materials science & engineering》 |2017年第9期|296-304|共9页
  • 作者单位

    School of Biological Science and Technology, University of Jinan. No. 336 West Road of Nanxinzhuang, Jinan 250022, Shandong Province, PR China;

    School of Medicine and Life Sciences, University of Jinan-Shandong Academy of Medical Sciences, No. 16866 East Road of Jingshi, Jinan 250200, Shandong Province, PR China,Shandong Academy of Medical Sciences, No. 18877Jingshi Road, Jinan 250062, Shandong Province, PR China;

    School of Biological Science and Technology, University of Jinan. No. 336 West Road of Nanxinzhuang, Jinan 250022, Shandong Province, PR China;

    School of Biological Science and Technology, University of Jinan. No. 336 West Road of Nanxinzhuang, Jinan 250022, Shandong Province, PR China;

    School of Biological Science and Technology, University of Jinan. No. 336 West Road of Nanxinzhuang, Jinan 250022, Shandong Province, PR China;

    School of Biological Science and Technology, University of Jinan. No. 336 West Road of Nanxinzhuang, Jinan 250022, Shandong Province, PR China;

    School of Biological Science and Technology, University of Jinan. No. 336 West Road of Nanxinzhuang, Jinan 250022, Shandong Province, PR China;

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  • 原文格式 PDF
  • 正文语种 eng
  • 中图分类
  • 关键词

    Skin delivery; Micelles; Antifungal agent; Ketoconazole;

    机译:皮肤输送;胶束;抗真菌剂;酮康唑;

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