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dc.contributor.authorMustafa, Natali Rianika
dc.contributor.authorSpelbos, Vincent Simon
dc.contributor.authorWitkamp, Geert Jan
dc.contributor.authorVerpoorte, Robert
dc.contributor.authorChoi, Young Hae
dc.date.accessioned2021-05-06T08:53:13Z
dc.date.available2021-05-06T08:53:13Z
dc.date.issued2021-04-30
dc.date.submitted2021-03-09
dc.identifier.citationMustafa, N. R., Spelbos, V. S., Witkamp, G.-J., Verpoorte, R., & Choi, Y. H. (2021). Solubility and Stability of Some Pharmaceuticals in Natural Deep Eutectic Solvents-Based Formulations. Molecules, 26(9), 2645. doi:10.3390/molecules26092645
dc.identifier.issn1420-3049
dc.identifier.pmid33946576
dc.identifier.doi10.3390/molecules26092645
dc.identifier.urihttp://hdl.handle.net/10754/669113
dc.description.abstractSome medicines are poorly soluble in water. For tube feeding and parenteral administration, liquid formulations are required. The discovery of natural deep eutectic solvents (NADES) opened the way to potential applications for liquid drug formulations. NADES consists of a mixture of two or more simple natural products such as sugars, amino acids, organic acids, choline/betaine, and poly-alcohols in certain molar ratios. A series of NADES with a water content of 0-30% (w/w) was screened for the ability to solubilize (in a stable way) some poorly water-soluble pharmaceuticals at a concentration of 5 mg/mL. The results showed that NADES selectively dissolved the tested drugs. Some mixtures of choline-based NADES, acid-neutral or sugars-based NADES could dissolve chloral hydrate (dissociated in water), ranitidine·HCl (polymorphism), and methylphenidate (water insoluble), at a concentration of up to 250 mg/mL, the highest concentration tested. Whereas a mixture of lactic-acid-propyleneglycol could dissolve spironolacton and trimethoprim at a concentration up to 50 and 100 mg/mL, respectively. The results showed that NADES are promising solvents for formulation of poorly water-soluble medicines for the development of parenteral and tube feeding administration of non-water-soluble medicines. The chemical stability and bioavailability of these drug in NADES needs further studies.
dc.description.sponsorshipThis work was possible through a collaboration with Tiofarma, Oud-Beijerland, The Netherlands, and a Horizon Valorization Project Grant (93515516) from Netherlands Genomics Initiative.
dc.publisherMDPI AG
dc.relation.urlhttps://www.mdpi.com/1420-3049/26/9/2645
dc.rightsThis article is an open access article distributed under the terms and conditions of the Creative Commons Attribution (CC BY) license.
dc.rights.urihttps://creativecommons.org/licenses/by/4.0/
dc.titleSolubility and Stability of Some Pharmaceuticals in Natural Deep Eutectic Solvents-Based Formulations.
dc.typeArticle
dc.contributor.departmentBiological and Environmental Science and Engineering (BESE) Division
dc.contributor.departmentEnvironmental Science and Engineering Program
dc.contributor.departmentWater Desalination and Reuse Research Center (WDRC)
dc.identifier.journalMolecules
dc.eprint.versionPublisher's Version/PDF
dc.contributor.institutionNatural Products Laboratory, Institute of Biology Leiden, Leiden University, 2333 Leiden, The Netherlands.
dc.contributor.institutionTiofarma, 3261 Oud-Beijerland, The Netherlands.
dc.contributor.institutionCollege of Pharmacy, Kyung Hee University, Seoul 02447, Korea.
dc.identifier.volume26
dc.identifier.issue9
dc.identifier.pages2645
kaust.personWitkamp, Geert Jan
dc.date.accepted2021-04-27
refterms.dateFOA2021-05-06T08:54:29Z


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This article is an open access article distributed under the terms and conditions of the Creative Commons Attribution (CC BY) license.
Except where otherwise noted, this item's license is described as This article is an open access article distributed under the terms and conditions of the Creative Commons Attribution (CC BY) license.