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Article

Solubility and Stability of Some Pharmaceuticals in Natural Deep Eutectic Solvents-Based Formulations

1
Natural Products Laboratory, Institute of Biology Leiden, Leiden University, 2333 Leiden, The Netherlands
2
Tiofarma, 3261 Oud-Beijerland, The Netherlands
3
Division of Biological and Environmental Sciences and Engineering, King Abdullah University of Science and Technology, KAUST4700, Thuwal 23955, Saudi Arabia
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College of Pharmacy, Kyung Hee University, Seoul 02447, Korea
*
Author to whom correspondence should be addressed.
Academic Editors: Tamar Greaves and Jorge F. B. Pereira
Molecules 2021, 26(9), 2645; https://doi.org/10.3390/molecules26092645
Received: 9 March 2021 / Revised: 22 April 2021 / Accepted: 27 April 2021 / Published: 30 April 2021
Some 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. View Full-Text
Keywords: natural deep eutectic solvents; pharmaceutical formulation; solubilization; stability; medicines natural deep eutectic solvents; pharmaceutical formulation; solubilization; stability; medicines
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MDPI and ACS Style

Mustafa, N.R.; Spelbos, V.S.; Witkamp, G.-J.; Verpoorte, R.; Choi, Y.H. Solubility and Stability of Some Pharmaceuticals in Natural Deep Eutectic Solvents-Based Formulations. Molecules 2021, 26, 2645. https://doi.org/10.3390/molecules26092645

AMA Style

Mustafa NR, Spelbos VS, Witkamp G-J, Verpoorte R, Choi YH. Solubility and Stability of Some Pharmaceuticals in Natural Deep Eutectic Solvents-Based Formulations. Molecules. 2021; 26(9):2645. https://doi.org/10.3390/molecules26092645

Chicago/Turabian Style

Mustafa, Natali R., Vincent S. Spelbos, Geert-Jan Witkamp, Robert Verpoorte, and Young H. Choi. 2021. "Solubility and Stability of Some Pharmaceuticals in Natural Deep Eutectic Solvents-Based Formulations" Molecules 26, no. 9: 2645. https://doi.org/10.3390/molecules26092645

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