Solubilization of cyclosporin A

Yingqing Ran, Luwei Zhao, Qing Xu, Samuel H. Yalkowsky

Research output: Contribution to journalArticle

54 Scopus citations

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 (α-cyclodextrin [(αCD)] and hydroxypropyl-β-cyclodextrin[(HPβCD)] 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 αCD was more effective than HPβCD. Cosolvents on the other hand did not increase the solubility of CsA as much as expected from the LOGP (logrithm of water-octanol partition coefficent) value of CsA.

Original languageEnglish (US)
Article number2
JournalAAPS PharmSciTech
Volume2
Issue number1
DOIs
StatePublished - 2001

Keywords

  • Conformation
  • Cyclosporin A
  • Solubility
  • Solubilzation

ASJC Scopus subject areas

  • Pharmaceutical Science

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