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In Vitro Evaluation of Self-Nano-Emulsifying Drug Delivery Systems (SNEDDS) Containing Room Temperature Ionic Liquids (RTILs) for the Oral Delivery of Amphotericin B.
Pharmaceutics ( IF 5.4 ) Pub Date : 2020-07-25 , DOI: 10.3390/pharmaceutics12080699
Eleni Kontogiannidou 1 , Thomas Meikopoulos 2 , Helen Gika 3 , Emmanuel Panteris 4 , Ioannis S Vizirianakis 5 , Anette Müllertz 6, 7 , Dimitrios G Fatouros 1
Affiliation  

Amphotericin B (AmpB), one of the most commonly used agents in the treatment of severe fungal infections and life-threatening parasitic diseases such as visceral Leishmaniasis, has a negligible oral bioavailability, primarily due to a low solubility and permeability. To develop an oral formulation, medium chain triglycerides and nonionic surfactants in a self-nano-emulsifying drug delivery system (SNEDDS) containing AmpB were combined with room temperature ionic liquids (RTILs) of imidazolium. The presence of ionic liquids significantly enhanced the solubility of AmpB, exhibited a low toxicity and increased the transport of AmpB across Caco-2 cell monolayers. The combination of RTILs with a lipid formulation might be a promising strategy to improve the oral bioavailability of AmpB.

中文翻译:

含室温离子液体(RTIL)的两性霉素B口服递送的自纳米乳化药物递送系统(SNEDDS)的体外评估。

两性霉素B(AmpB)是治疗严重真菌感染和威胁生命的寄生虫病(例如内脏利什曼病)的最常用药物之一,其口服生物利用度可忽略不计,主要是由于其低溶解度和渗透性。为了开发口服制剂,将含有AmpB的自纳米乳化药物递送系统(SNEDDS)中的中链甘油三酸酯和非离子表面活性剂与咪唑鎓的室温离子液体(RTIL)混合。离子液体的存在显着增强了AmpB的溶解度,显示出低毒性并增加了AmpB在Caco-2细胞单层中的转运。RTILs与脂质制剂的组合可能是改善AmpB口服生物利用度的有前途的策略。
更新日期:2020-07-25
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