Mapping the pharmaceutical design space by amorphous ionic liquid strategies

Journal of Controlled Release : Official Journal of the Controlled Release Society
Johannes WiestLorenz Meinel

Abstract

Poor water solubility of drugs fuels complex formulations and jeopardizes patient access to medication. Simplifying these complexities we systematically synthesized a library of 36 sterically demanding counterions and mapped the pharmaceutical design space for amorphous ionic liquid strategies for Selurampanel, a poorly water soluble drug used against migraine. Patients would benefit from a rapid uptake after oral administration to alleviate migraine symptoms. Therefore, we probed the ionic liquids for the flux, supersaturation period and hygroscopicity leading to algorithms linking molecular counterion descriptors to predicted pharmaceutical outcome. By that, 30- or 800-fold improvements of the supersaturation period and fluxes were achieved as were immediate to sustained release profiles through structural counterions' optimization compared to the crystalline free acid of Selurampanel. Guided by ionic liquid structure, in vivo profiles ranged from rapid bioavailability and high maximal plasma concentrations to sustained patterns. In conclusion, the study outlined and predicted the accessible pharmaceutical design space of amorphous ionic liquid based and excipient-free formulations pointing to the enormous pharmaceutical pote...Continue Reading

Citations

Apr 24, 2019·The Journal of Pharmacology and Experimental Therapeutics·G KaurM N V Ravi Kumar
Dec 18, 2020·Journal of Controlled Release : Official Journal of the Controlled Release Society·Jonas SchlauersbachLorenz Meinel
Jul 22, 2018·Journal of Controlled Release : Official Journal of the Controlled Release Society·Eden E L TannerSamir Mitragotri
Jul 11, 2021·Advanced Science·Alexander M CurreriEden E L Tanner
Aug 24, 2021·Journal of Controlled Release : Official Journal of the Controlled Release Society·Xiying WuJianping Qi

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