AAPS PharmSciTech

, Volume 2, Issue 1, pp 23–26 | Cite as

Solubilization of cyclosporin A

  • Yingqing Ran
  • Luwei Zhao
  • Qing Xu
  • Samuel H. Yalkowsky
Article

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[(HP\CD)] 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 HP\CD. Cosolvents on the other hand did not increase the solubility of CsA as much as expected from the LOGP (logrithm of wateroctanol partition coefficent) value of CsA.

KeyWords

Cyclosporin A Conformation Solubility Solubilization 

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Copyright information

© American Association of Pharmaceutical Scientists 2001

Authors and Affiliations

  • Yingqing Ran
    • 1
  • Luwei Zhao
    • 2
  • Qing Xu
    • 3
  • Samuel H. Yalkowsky
    • 1
  1. 1.Department of Pharmaceutical Sciences; College of PharmacyThe University of ArizonaTucson
  2. 2.Aventis Pharmaceuticals CompanyBridgewater
  3. 3.Department of ChemistryThe University of ArizonaTucson

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