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Preparation, Characterization, and Formulation Optimization of Ionic-Liquid-in-Water Nanoemulsions toward Systemic Delivery of Amphotericin B.
Molecular Pharmaceutics ( IF 4.5 ) Pub Date : 2020-04-28 , DOI: 10.1021/acs.molpharmaceut.9b00809 Moira M Esson 1 , Sandro Mecozzi 1, 2
Molecular Pharmaceutics ( IF 4.5 ) Pub Date : 2020-04-28 , DOI: 10.1021/acs.molpharmaceut.9b00809 Moira M Esson 1 , Sandro Mecozzi 1, 2
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Amphotericin B (AmB) is an antifungal agent that poses a challenge for intravenous drug delivery due to its hydrophobicity and severe side effects that are attributed to the self-aggregation of AmB in aqueous solution. To overcome this problem, we have rationally designed an ionic-liquid-in-water nanoemulsion drug delivery system that harnesses the unique properties of ionic liquids. The complex drug AmB serves as a model pharmaceutical agent to demonstrate the robustness of ionic-liquid-in-water nanoemulsions. High concentrations of AmB were solubilized in a new hydrophobic dicholinium-based ionic liquid. The absorption spectrum of AmB in an ionic liquid mixture and prepared nanoemulsion indicates AmB solubilization in the monomeric form. The hydrophobic ionic liquid exhibits high in vivo biocompatibility with zebrafish. The hemolytic activity of the AmB nanoemulsion was negligible, yet it maintained antifungal activity against Candida albicans. The preliminary results presented in this Communication indicate that ionic-liquid-in-water nanoemulsions may allow for the delivery of a variety of pharmaceuticals intravenously, broadening the scope of ionic liquids in the pharmaceutical sciences.
中文翻译：
离子液体水纳米乳剂对两性霉素B的全身释放的制备，表征和配方优化。
两性霉素B（AmB）是一种抗真菌剂，由于其疏水性和严重的副作用（这归因于AmB在水溶液中的自聚集作用），对静脉内给药构成了挑战。为了克服这个问题，我们合理设计了一种离子水包纳米乳剂给药系统，该系统利用了离子液体的独特性能。复合药物AmB用作模型药剂，以证明离子液体在水中的纳米乳剂的耐用性。高浓度的AmB溶解在一种新的疏水性基于二氯胆碱的离子液体中。AmB在离子液体混合物和制备的纳米乳液中的吸收光谱表明，AmB以单体形式溶解。疏水离子液体在体内表现出很高的与斑马鱼的生物相容性。AmB纳米乳剂的溶血活性可以忽略不计，但仍保持了对白色念珠菌的抗真菌活性。该来文中显示的初步结果表明，水中离子液体纳米乳剂可允许静脉内输送多种药物，从而扩大了离子液体在药学领域的范围。
更新日期：2020-04-28
中文翻译：
离子液体水纳米乳剂对两性霉素B的全身释放的制备，表征和配方优化。
两性霉素B（AmB）是一种抗真菌剂，由于其疏水性和严重的副作用（这归因于AmB在水溶液中的自聚集作用），对静脉内给药构成了挑战。为了克服这个问题，我们合理设计了一种离子水包纳米乳剂给药系统，该系统利用了离子液体的独特性能。复合药物AmB用作模型药剂，以证明离子液体在水中的纳米乳剂的耐用性。高浓度的AmB溶解在一种新的疏水性基于二氯胆碱的离子液体中。AmB在离子液体混合物和制备的纳米乳液中的吸收光谱表明，AmB以单体形式溶解。疏水离子液体在体内表现出很高的与斑马鱼的生物相容性。AmB纳米乳剂的溶血活性可以忽略不计，但仍保持了对白色念珠菌的抗真菌活性。该来文中显示的初步结果表明，水中离子液体纳米乳剂可允许静脉内输送多种药物，从而扩大了离子液体在药学领域的范围。
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