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Cyclodextrins as pharmaceutical solubilizers.

Marcus E Brewster1, Thorsteinn Loftsson

  • 1Chemical and Pharmaceutical Development, Johnson & Johnson Pharmaceutical Research and Development, Janssen Pharmaceutica, Turnhoutseweg 30, B-2340 Beerse, Belgium. mbrewste@prdbe.jnj.com

Advanced Drug Delivery Reviews
|July 3, 2007
PubMed
Summary
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Cyclodextrins enhance drug solubility and bioavailability by forming complexes with poorly soluble drugs. This review explores their mechanisms and analytical tools for studying drug solubilization.

Area of Science:

  • Pharmaceutical Sciences
  • Physical Chemistry

Background:

  • Cyclodextrins are versatile excipients widely used in pharmaceuticals.
  • Their popularity stems from the ability to improve the solubility of poorly water-soluble drugs.

Purpose of the Study:

  • To provide an overview of cyclodextrins as solubilizing agents.
  • To highlight kinetic and thermodynamic tools for studying drug solubilization by cyclodextrins.

Main Methods:

  • Review of literature on cyclodextrin-drug interactions.
  • Discussion of inclusion and non-inclusion complex formation.
  • Exploration of aggregate formation and stabilization of supersaturated solutions.

Main Results:

  • Cyclodextrins increase apparent drug water solubility via non-covalent complexation.

Related Experiment Videos

  • Enhanced solubility improves dissolution rates and oral bioavailability for BCS Class II and IV drugs.
  • Cyclodextrins can mask undesirable drug physicochemical properties.

    • Conclusions:

    • Cyclodextrins are effective solubilizers for poorly water-soluble drugs.
    • Understanding the thermodynamics and kinetics of complexation is crucial for drug development.
    • Cyclodextrin technology enables the formulation of challenging drug candidates.