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Open AccessArticle

Choline-Amino Acid Ionic Liquids as Green Functional Excipients to Enhance Drug Solubility

1
CBIOS-Universidade Lusófona’s Research Center for Biosciences & Health Technologies, Campo Grande 376, 1749-024 Lisboa, Portugal
2
Department of Biomedical Sciences, University of Alcalá, Ctra. Madrid-Barcelona Km. 33.600, Alcalá de Henares, 28871 Madrid, Spain
3
Department of Pharmacy, School of Pharmaceutical Sciences, University of São Paulo, 580 Prof. Lineu Prestes Av., Bl. 15, São Paulo, SP 05508-900, Brazil
4
Centro de Química e Bioquímica, Faculdade de Ciências, Universidade de Lisboa, 1749-016 Lisboa, Portugal
5
Research Institute for Medicines (iMed.ULisboa), Faculty of Pharmacy, Universidade de Lisboa, Av. Professor Gama Pinto, 1649-003 Lisboa, Portugal
*
Author to whom correspondence should be addressed.
Both authors contributed equally to the senior authorship.
Pharmaceutics 2018, 10(4), 288; https://doi.org/10.3390/pharmaceutics10040288
Received: 14 November 2018 / Revised: 12 December 2018 / Accepted: 15 December 2018 / Published: 19 December 2018
(This article belongs to the Special Issue New Approaches to Enhance Drug Solubility and Bioavailability)
The development of effective forms to incorporate poorly soluble drugs into delivery systems remains a problem. Thus, it is important to find alternatives such as finding excipients that increase drug solubility. Ionic liquids (ILs), particularly choline-based ILs, have been studied as solubility enhancers in drug delivery systems. Nonetheless, to acknowledge this property as a functionality, it needs to be proven at non-toxic concentrations. Hence, herein two choline-amino acid ILs were studied as functional excipients by evaluating their influence on the solubility of the poorly water-soluble ferulic acid and rutin, while considering their safety. The solubility of the drugs was always higher in the presence of the ILs than in water. Ionic liquids did not affect the radical scavenging activity of the drugs or the cell viability. Moreover, stable oil-in-water (O/W) emulsions were prepared containing each drug and the ILs, allowing a significantly higher drug loading. Globally, our results suggest that choline-based ILs may act as green functional excipients, since at non-toxic concentrations they considerably improve drug solubility/loading, without influencing the antioxidant activity of the drugs, the cell viability, or the stability of the formulations. View Full-Text
Keywords: ionic liquids; solubility/loading enhancement; radical scavenging activity; cell viability; oil-in-water emulsions; stability ionic liquids; solubility/loading enhancement; radical scavenging activity; cell viability; oil-in-water emulsions; stability
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MDPI and ACS Style

Caparica, R.; Júlio, A.; Baby, A.R.; Araújo, M.E.M.; Fernandes, A.S.; Costa, J.G.; Santos de Almeida, T. Choline-Amino Acid Ionic Liquids as Green Functional Excipients to Enhance Drug Solubility. Pharmaceutics 2018, 10, 288.

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