Publication Type Journal Article
Title Choline- versus imidazole-based ionic liquids as functional ingredients in topical delivery systems: cytotoxicity, solubility, and skin permeation studies
Authors Tania Santos de Almeida Ana Julio Nuno Saraiva Ana Sofia Fernandes M. Eduarda Araújo Andre Rolim Baby Catarina Rosado Joana Portugal Mota
Groups HC
Journal DRUG DEVELOPMENT AND INDUSTRIAL PHARMACY
Year 2017
Month
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Volume 43
Number 11
Pages 1858-1865
Abstract Background: Poor drug solubility represents a problem for the development of topical formulations. Since ionic liquids (ILs) can be placed in either lipophilic or hydrophilic solutions, they may be advantageous vehicles in such delivery systems. Nonetheless, it is vital to determine their usefulness when used at concentrations were cell viability is maintained, which was considered herein. Method: Five different ILs were prepared-three imidazole-based ILs: [C2mim][Br], [C4mim][Br], and [C6mim][Br]; and two choline-based ILs: [Cho][Phe] and [Cho][Glu]. Their cytotoxicity in human keratinocytes (HaCat cells), their influence in drug solubility and in percutaneous permeation, using pig skin membranes, was evaluated. Results: Caffeine and salicylic acid were used as model actives. Choline-based ILs proved to be more suitable as functional ingredients, since they showed higher impact on drug solubility and a lower cytotoxicity. The major solubility enhancement was observed for caffeine and further solubility studies were carried out with this active in several concentrations of the choline-based ILs (0.1; 0.2; 0.5; 1.0; 3.0 and 5.0\%, w/ w) at 25 degrees C and 32 degrees C. Solubility was greatly influenced by concentrations up to 0.5\%. The choline-based ILs showed no significant impact on the skin permeation, for both actives. The size of the imidazole-based ILs alkyl chain enhances the caffeine solubility and permeation, but also the ILs cytotoxicity. Stable O/W emulsions and gels were prepared containing the less toxic choline-based ILs and caffeine. Conclusions: Our results indicate that the choline-based ILs were effective functional ingredients, since, when used at nontoxic concentrations, they allowed a higher drug loading, while maintaining the stability of the formulations.
DOI http://dx.doi.org/10.1080/03639045.2017.1349788
ISBN
Publisher
Book Title
ISSN 0363-9045
EISSN 1520-5762
Conference Name
Bibtex ID ISI:000408947400011
Observations
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