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Solubility of Cyclodextrins and Drug/Cyclodextrin Complexes

Solubility of Cyclodextrins and Drug/Cyclodextrin Complexes


Title: Solubility of Cyclodextrins and Drug/Cyclodextrin Complexes
Author: Saokham, Phennapha
Muankaew, Chutimon
Jansook, Phatsawee
Loftsson, Thorsteinn   orcid.org/0000-0002-9439-1553
Date: 2018-05-11
Language: English
Scope: 1161
University/Institute: Háskóli Íslands
University of Iceland
School: Heilbrigðisvísindasvið (HÍ)
School of Health Sciences (UI)
Department: Lyfjafræðideild (HÍ)
Faculty of Pharmaceutical Sciences (UI)
Series: Molecules;23(5)
ISSN: 1420-3049
DOI: 10.3390/molecules23051161
Subject: Cyclodextrin; Solubility; Poorly soluble drug; Lyfjafræði; Lyfjaefnafræði
URI: https://hdl.handle.net/20.500.11815/1105

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Citation:

Saokham, P., Muankaew, C., Jansook, P., & Loftsson, T. (2018). Solubility of Cyclodextrins and Drug/Cyclodextrin Complexes. Molecules, 23(5), 1161. doi:10.3390/molecules23051161

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.

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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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