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.

journal_name

AAPS PharmSciTech

journal_title

AAPS PharmSciTech

authors

Ran Y,Zhao L,Xu Q,Yalkowsky SH

doi

10.1208/pt020102

keywords:

subject

Has Abstract

pub_date

2001-01-18 00:00:00

pages

E2

issue

1

issn

1530-9932

journal_volume

2

pub_type

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