Abstract
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.
Highlights
Lipid-based formulations are emerging as an interesting formulation strategy for providing bioavailability-enhancing mechanisms for poorly water-soluble drugs belonging to Biopharmaceutics Classification System (BCS) Class II or IV [1,2]
Three different room temperature ionic liquids (RTILs) were incorporated into the Self-nano-emulsifying drug delivery systems (SNEDDS) preconcentrates as follows: 0.3 g of IL was mixed with 0.7 g of SNEDDS), and they were stirred until complete homogenization (SNEDDS:BMIMBF4, SNEDDS:BMIMPF6 and SNEDDS:Hexyl-3-methylimidazolium chloride (HMIMCl)), forming clear isotropic preconcentrates
The ability of RTILs to increase solubility depends on their anions (PF6−, BF4−, Cl−) and the length of their alkyl chain
Summary
Lipid-based formulations are emerging as an interesting formulation strategy for providing bioavailability-enhancing mechanisms for poorly water-soluble drugs belonging to Biopharmaceutics Classification System (BCS) Class II or IV [1,2]. The oral delivery of these drugs is affected by their low bioavailability and lack of dose solubility [3]. Another important factor that affects the oral bioavailability of BCS IV drugs is poor intestinal permeability [3]. To enhance their solubility, lipid-based formulations have been successfully used as oral delivery systems [4]. Self-nano-emulsifying drug delivery systems (SNEDDS) are one of the most special and interesting lipid-based formulations [4] and are considered as a promising approach for improving the rate and extent of absorption of BCS II or IV drugs [5,6]. SNEDDS induce the formation of oil droplets, which in turn may facilitate the transport of the active across the intestinal membrane [11]
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