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Molecules 2018, 23(5), 1161; https://doi.org/10.3390/molecules23051161

Solubility of Cyclodextrins and Drug/Cyclodextrin Complexes

1
Faculty of Pharmacy, Rangsit University, Pathum Thani 12000, Thailand
2
Faculty of Pharmacy, Siam University, 38 Petchkasem Road, Phasi Charoen District, Bangkok 10160, Thailand
3
Faculty of Pharmaceutical Sciences, Chulalongkorn University, 254 Phyathai Road, Pathumwan, Bangkok 10330, Thailand
4
Faculty of Pharmaceutical Sciences, University of Iceland, Hofsvallagata 53, 107 Reykjavik, Iceland
These authors contributed equally to this work.
*
Author to whom correspondence should be addressed.
Academic Editor: Dr. Bernard Martel
Received: 13 April 2018 / Revised: 7 May 2018 / Accepted: 8 May 2018 / Published: 11 May 2018
(This article belongs to the Special Issue Cyclodextrin Chemistry 2018)
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Abstract

Cyclodextrins (CDs), a group of oligosaccharides formed by glucose units bound together in a ring, show a promising ability to form complexes with drug molecules and improve their physicochemical properties without molecular modifications. The stoichiometry of drug/CD complexes is most frequently 1:1. However, natural CDs have a tendency to self-assemble and form aggregates in aqueous media. CD aggregation can limit their solubility. Through derivative formation, it is possible to enhance their solubility and complexation capacity, but this depends on the type of substituent and degree of substitution. Formation of water-soluble drug/CD complexes can increase drug permeation through biological membranes. To maximize drug permeation the amount of added CD into pharmaceutical preparation has to be optimized. However, solubility of CDs, especially that of natural CDs, is affected by the complex formation. The presence of pharmaceutical excipients, such as water-soluble polymers, preservatives, and surfactants, can influence the solubilizing abilities of CDs, but this depends on the excipients’ physicochemical properties. The competitive CD complexation of drugs and excipients has to be considered during formulation studies. View Full-Text
Keywords: cyclodextrin; complex; solubility; poorly soluble drug cyclodextrin; complex; solubility; poorly soluble drug
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This is an open access article distributed under the Creative Commons Attribution License which permits unrestricted use, distribution, and reproduction in any medium, provided the original work is properly cited. (CC BY 4.0).
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Saokham, P.; Muankaew, C.; Jansook, P.; Loftsson, T. Solubility of Cyclodextrins and Drug/Cyclodextrin Complexes. Molecules 2018, 23, 1161.

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