NDLI: Ionic Liquid Versus Prodrug Strategy to Address Formulation Challenges

Content Provider	Springer Nature Link
Author	Balk, Anja Widmer, Toni Wiest, Johannes Bruhn, Heike Rybak, Jens Christoph Matthes, Philipp Müller Buschbaum, Klaus Sakalis, Anastasios Lühmann, Tessa Berghausen, Jörg Holzgrabe, Ulrike Galli, Bru Meinel, Lorenz
Copyright Year	2014
Abstract	A poorly water soluble acidic active pharmaceutical ingredient (API) was transformed into an ionic liquid (IL) aiming at faster and higher oral availability in comparison to a prodrug.API preparations were characterized in solid state by single crystal and powder diffraction, NMR, DSC, IR and in solution by NMR and ESI-MS. Dissolution and precipitation kinetics were detailed as was the role of the counterion on API supersaturation. Transepithelial API transport through Caco-2 monolayers and counterion cytotoxicity were assessed.The mechanism leading to a 700 fold faster dissolution rate and longer duration of API supersaturation of the ionic liquid in comparison to the free acid was deciphered. Transepithelial transport was about three times higher for the IL in comparison to the prodrug when substances were applied as suspensions with the higher solubility of the IL outpacing the higher permeability of the prodrug. The counterion was nontoxic with IC$_{50}$ values in the upper μM / lower mM range in cell lines of hepatic and renal origin as well as in macrophages.The IL approach was instrumental for tuning physico-chemical API properties, while avoiding the inherent need for structural changes as required for prodrugs. Graphical Abstract Stabilization of API in solution by Ionic liquid formation
Starting Page	2154
Ending Page	2167
Page Count	14
File Format	PDF
ISSN	07248741
Journal	Pharmaceutical Research
Volume Number	32
Issue Number	6
e-ISSN	1573904X
Language	English
Publisher	Springer US
Publisher Date	2014-12-23
Publisher Place	New York
Access Restriction	One Nation One Subscription (ONOS)
Subject Keyword	Pharmacology/Toxicology Pharmacy Biochemistry Medical Law Biomedical Engineering
Content Type	Text
Resource Type	Article
Subject	Organic Chemistry Pharmacology Molecular Medicine Pharmacology (medical) Biotechnology Pharmaceutical Science

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