Complexation of statins with β-cyclodextrin in solutions of small molecular additives and macromolecular colloids

András Süle, F. Csempesz

Research output: Chapter in Book/Report/Conference proceedingConference contribution

3 Citations (Scopus)

Abstract

The solubility of lovastatin and simvastatin (inevitable drugs in the management of cardiovascular diseases) was studied by phase-solubility measurements in multicomponent colloidal and non-colloidal media. Complexation in aqueous solutions of the highly lipophilic statins with β-cyclodextrin (β-CD) in the absence and the presence of dissolved polyvinyl pyrrolidone, its monomeric compound, tartaric acid and urea, respectively, were investigated. For the characterization of the CD-statin inclusion complexes, stability constants for the associates have been calculated. It was shown that complexation might lead to considerable improvement of the aqueous solubilities of both statins. In binary systems dominantly statin-β-CD associates of 1:1 molar ratios form, which exhibit considerable surface activity. In statin-CD-additive ternary systems the solubility of the statins could be further improved. The enhanced drug solubilities in the solutions of small molecular mass solutes are likely related due to the peculiar feature of the additives to destroy the H-bonding system of β-CD. In polymer-containing systems statin-CD-polymer associates of supramolecular structure may presumably form in a way that portions of surface-active statin-β-CD complexes are anchored at the macromolecular chains.

Original languageEnglish
Title of host publicationProgress in Colloid and Polymer Science
Pages93-100
Number of pages8
Volume135
DOIs
Publication statusPublished - 2008

Publication series

NameProgress in Colloid and Polymer Science
Volume135
ISSN (Print)0340255X

Fingerprint

Hydroxymethylglutaryl-CoA Reductase Inhibitors
Cyclodextrins
Colloids
Complexation
colloids
solubility
Solubility
drugs
polymers
Molecular mass
Polymers
Ternary systems
ternary systems
ureas
Urea
Polyvinyls
solutes
Pyrrolidinones
Lovastatin
Simvastatin

Keywords

  • Cyclodextrins
  • Dissolution
  • Inclusion complexes
  • Macromolecular colloids
  • Statins
  • Supramolecular associates

ASJC Scopus subject areas

  • Organic Chemistry
  • Physical and Theoretical Chemistry
  • Colloid and Surface Chemistry
  • Materials Chemistry
  • Polymers and Plastics

Cite this

Süle, A., & Csempesz, F. (2008). Complexation of statins with β-cyclodextrin in solutions of small molecular additives and macromolecular colloids. In Progress in Colloid and Polymer Science (Vol. 135, pp. 93-100). (Progress in Colloid and Polymer Science; Vol. 135). https://doi.org/10.1007/2882-2008-120

Complexation of statins with β-cyclodextrin in solutions of small molecular additives and macromolecular colloids. / Süle, András; Csempesz, F.

Progress in Colloid and Polymer Science. Vol. 135 2008. p. 93-100 (Progress in Colloid and Polymer Science; Vol. 135).

Research output: Chapter in Book/Report/Conference proceedingConference contribution

Süle, A & Csempesz, F 2008, Complexation of statins with β-cyclodextrin in solutions of small molecular additives and macromolecular colloids. in Progress in Colloid and Polymer Science. vol. 135, Progress in Colloid and Polymer Science, vol. 135, pp. 93-100. https://doi.org/10.1007/2882-2008-120
Süle A, Csempesz F. Complexation of statins with β-cyclodextrin in solutions of small molecular additives and macromolecular colloids. In Progress in Colloid and Polymer Science. Vol. 135. 2008. p. 93-100. (Progress in Colloid and Polymer Science). https://doi.org/10.1007/2882-2008-120
Süle, András ; Csempesz, F. / Complexation of statins with β-cyclodextrin in solutions of small molecular additives and macromolecular colloids. Progress in Colloid and Polymer Science. Vol. 135 2008. pp. 93-100 (Progress in Colloid and Polymer Science).
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AB - The solubility of lovastatin and simvastatin (inevitable drugs in the management of cardiovascular diseases) was studied by phase-solubility measurements in multicomponent colloidal and non-colloidal media. Complexation in aqueous solutions of the highly lipophilic statins with β-cyclodextrin (β-CD) in the absence and the presence of dissolved polyvinyl pyrrolidone, its monomeric compound, tartaric acid and urea, respectively, were investigated. For the characterization of the CD-statin inclusion complexes, stability constants for the associates have been calculated. It was shown that complexation might lead to considerable improvement of the aqueous solubilities of both statins. In binary systems dominantly statin-β-CD associates of 1:1 molar ratios form, which exhibit considerable surface activity. In statin-CD-additive ternary systems the solubility of the statins could be further improved. The enhanced drug solubilities in the solutions of small molecular mass solutes are likely related due to the peculiar feature of the additives to destroy the H-bonding system of β-CD. In polymer-containing systems statin-CD-polymer associates of supramolecular structure may presumably form in a way that portions of surface-active statin-β-CD complexes are anchored at the macromolecular chains.

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