Developing a universal
drug delivery vehicle of sparingly soluble
drugs remains a challenge, with surface-active ionic liquid (SAIL)-based
ionic liquid-in-oil (IL/O) microemulsions (MEs) being the most suitable
vehicles. In this study, a series of SAILs were formulated to prepare
novel IL/O MEs composed of SAIL, sorbitan laurate (Span-20), and isopropyl
myristate. On the basis of the constructed pseudoternary diagrams,
the SAILs played vital surfactant roles with Span-20 acting as a cosurfactant.
Excellent drug solubility of MEs prepared with a ratio of 2:1 (SAIL[Cho][Ole]:Span-20)
was observed. Examination of the droplet shape, size, and size distribution
of the MEs revealed well-distributed particle sizes of 6.5–21.2
nm that formed spherical micelles with the IL 1,3-dimethylimidazolium
dimethyl phosphate at the core of the MEs. The MEs showed excellent
solubility of sparingly soluble drugs (i.e., celecoxib, acyclovir,
methotrexate, and dantrolene sodium). In vitro cytotoxicity of the
new carrier using a three-dimensional reconstructed human epidermis
model revealed that the cell viability of SAIL-based MEs (94%) was
similar when compared to conventional Tween-80-based MEs (96%) at
the same IL concentration (4%). The results indicate that the SAIL
surfactant in the MEs represents a potential alternative to conventional
surfactants for solubilizing insoluble drug molecules.