Ionic liquid-assisted transdermal delivery of sparingly soluble drugs

Abstract

We report the first successful application of a novel IL-assisted non-aqueous microemulsion stabilized by a blend of two nontoxic surfactants, polyoxyethylene sorbitan monooleate (Tween-80), and sorbitan laurate (Span-20) for transdermal delivery of acyclovir, which is insoluble or sparingly soluble in water and most common organic liquids.

Development of Novel Ionic Liquid-Based Microemulsion Formulation for Dermal Delivery of 5-Fluorouracil

“…Previous reports illustrate attempts on dermal delivery of poorly soluble drugs using IL-based carrier system (7,17). In contrast to this, we propose to develop a novel IL-based carrier system for a water-soluble BCS class III drug 5-fluorouracil (5-FU), which is soluble in water, but the permeation through skin is the rate-limiting factor of this drug (19).…”

“…The surfactants containing longer saturated alkyl chain (Tween 20, Tween 40, and Tween 60) may not exhibit the required fluidity for ME formation as compared to Tween 80 which contains a double bond in its lipophilic chain. The choice of Tween 80 as surfactant was also based on the fact that Tween 80 has hydrophilic polyoxyethylene (PEO) groups, which have a strong affinity with the imidazolium cation appended in ILs through the electrostatic interaction (39). Therefore, on the basis of drug solubility (Table III) and emulsification capability, Tween 80 was selected as the surfactant for formulating MEs.…”

“…Another study reports the influence of the type of ILs on the formation and drug encapsulation efficiency of IL/o MEs (17). It was observed that such ionic liquid-based MEs are capable of solubilizing higher amount of poorly soluble drugs like a c y c l o v i r , m e t h o t r e x a t e , a n d 1 -[ ( 5 -( p -n i t r ophenyl)furfurylidene)amino]hydantoin sodium than their individual components and water.…”

Nonaqueous Microemulsions Containing Ionic Liquids – Properties and Applications

“…Moreover, we could demonstrate that biodiesel can act as oil phase in high temperature microemulsions highlighting a way towards the formulation of biocompatible microemulsions (Zech et al, 2010 c (Moniruzzaman et al, 2010). A large number of drugs are sparingly soluble in both water and most organic solvents.…”

Hydrophilic Ionic Liquids as Ingredients of Gel-Based Dermal Formulations

“…However, only a few studies have been published regarding the use of ILs in pharmaceutical or cosmetic applications so far. ILs were used mostly in microemulsions (14) as oil substitutes, water substitutes, additives, or surfactants (15)(16)(17). Multiple emulsions containing ILs as a hydrophobic phase have also been reported (18).…”