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AAPS PharmSciTech
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AAPS PharmSciTech
Article . 2001 . Peer-reviewed
License: Springer TDM
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AAPS PharmSciTech
Article . 2004
Data sources: Europe PubMed Central
AAPS PharmSciTech
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Solubilization of cyclosporin A

descriptionPublicationkeyboard_double_arrow_right Article 01 Mar 2001Publisher:Springer Science and Business Media LLCJournal:AAPS PharmSciTech, volume 2, pages 23-26 (eissn: 1530-9932, Copyright policy )
Authors: Yingqing Ran; Samuel H. Yalkowsky; Qing Xu; Luwei Zhao;

doi: 10.1208/pt020102

pmid: 14727890

pmc: PMC2750256

Solubilization of cyclosporin A

Abstract

This study investigated the solubilization of cyclosporin A (CsA), a neutral undecapeptide, by cosolvency, micellization, and complexation. Cosolvents (ethanol, propylene glycol, polyethylene glycol, tetrahydrofurfuryl alcohol polyethyleneglycol ether, and glycerin), surfactants (polyoxyethylene sorbitan monooleate [(Tween 80)], polyoxyethylene sorbitan monolaurate [(Tween 20)], and Cremophor EL), and cyclodextrins (alpha-cyclodextrin [(alphaCD)] and hydroxypropyl-beta-cyclodextrin[(HPbetaCD)] were used as solubilizing agents in this study. Surfactants had a noticeable effect in increasing CsA solubility. Twenty percent solutions of Tween 20, Tween 80, and Cremophor EL increased the solubility by 60 to 160 fold. Cyclodextrins can increase the CsA solubility, but alphaCD was more effective than HPbetaCD. Cosolvents on the other hand did not increase the solubility of CsA as much as expected from the LOGP (logarithm of water-octanol partition coefficient) value of CsA.

Related Organizations
Keywords

Solutions, Cyclodextrins, Surface-Active Agents, Drug Stability, Models, Chemical, Solubility, Chemistry, Pharmaceutical, Cyclosporine, Solvents, Micelles

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    popularity
    This indicator reflects the "current" impact/attention (the "hype") of an article in the research community at large, based on the underlying citation network.
    		 Top 10%
    influence
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    This indicator reflects the initial momentum of an article directly after its publication, based on the underlying citation network.
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citations
This is an alternative to the "Influence" indicator, which also reflects the overall/total impact of an article in the research community at large, based on the underlying citation network (diachronically).
BIP!Citations provided by BIP!
popularity
This indicator reflects the "current" impact/attention (the "hype") of an article in the research community at large, based on the underlying citation network.
BIP!Popularity provided by BIP!
influence
This indicator reflects the overall/total impact of an article in the research community at large, based on the underlying citation network (diachronically).
BIP!Influence provided by BIP!
impulse
This indicator reflects the initial momentum of an article directly after its publication, based on the underlying citation network.
BIP!Impulse provided by BIP!
53
Top 10%
Top 10%
Average
bronze