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Cyclodextrins as functional excipients: methods to enhance complexation efficiency.

Thorsteinn Loftsson1, Marcus E Brewster

  • 1Faculty of Pharmaceutical Sciences, University of Iceland, IS-107 Reykjavik, Iceland. thorstlo@hi.is

Journal of Pharmaceutical Sciences
|February 16, 2012
PubMed
Summary
This summary is machine-generated.

Cyclodextrins enhance drug solubility, but their bulk limits solid dosage forms. Manipulating complexation efficiency (CE) can expand their use in tablets for more potent drugs.

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Area of Science:

  • Pharmaceutical Sciences
  • Drug Delivery
  • Physical Chemistry

Background:

  • Cyclodextrins are versatile solubilizing excipients with numerous applications.
  • Their use in solid dosage forms is limited by formulation bulk, especially for non-potent drugs.
  • Enhancing cyclodextrin complexation efficiency (CE) is key to expanding their utility.

Purpose of the Study:

  • To review strategies for increasing the complexation efficiency (CE) of cyclodextrins with drugs.
  • To discuss factors influencing CE, including drug ionization, salt form, and excipient interactions.
  • To explore mechanisms like aggregation and complex formation impacting cyclodextrin utility.

Main Methods:

  • Literature review of tools and materials for enhancing cyclodextrin CE.
  • Analysis of drug solubility (S(0)) and phase-solubility isotherm slope.
  • Discussion of polymer, charge, and supersaturation effects on complexation.

Main Results:

  • Drug ionization, salt use, and polymers significantly impact CE.
  • Charge interactions and shielding play crucial roles in complex formation.
  • Supersaturation and drug form influence the mechanisms of complexation.

Conclusions:

  • Optimizing CE through various strategies can overcome limitations of cyclodextrins in solid dosage forms.
  • Understanding complexation mechanisms is vital for effective drug formulation.
  • This approach broadens the application of cyclodextrins for a wider range of drugs.