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Cyclodextrins: structure, physicochemical properties and pharmaceutical applications.

Phatsawee Jansook1, Noriko Ogawa2, Thorsteinn Loftsson3

  • 1Department of Pharmaceutics and Industrial Pharmacy, Faculty of Pharmaceutical Sciences, Chulalongkorn University, 254 Phyathai Road, Wangmai, Pathumwan, Bangkok 10330, Thailand.

International Journal of Pharmaceutics
|November 16, 2017
PubMed
Summary
This summary is machine-generated.

Cyclodextrins (CDs) are versatile pharmaceutical excipients that improve drug solubility and bioavailability. This review covers methods to optimize CD formulations for enhanced drug delivery across various administration routes.

Keywords:
AggregatesAqueous solutionCyclodextrinsInclusion complexPharmaceuticalSolubilityWater-insoluble drugs

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Area of Science:

  • Pharmaceutical Science
  • Drug Delivery
  • Supramolecular Chemistry

Background:

  • Cyclodextrins (CDs) are widely studied cyclic oligosaccharides with over a century of research.
  • They are utilized as pharmaceutical excipients to enhance solubility, permeability, and bioavailability of poorly soluble drugs.
  • Natural CDs and derivatives are also used in food, toiletry products, and have pharmacopeial monographs.

Purpose of the Study:

  • To review methods for investigating cyclodextrin aggregate formation.
  • To explore techniques for increasing the solubilizing effects of cyclodextrins.
  • To discuss the role of cyclodextrins in various pharmaceutical formulations and administration routes.

Main Methods:

  • Review of literature on cyclodextrin aggregate formation.
  • Analysis of techniques to enhance drug solubility and complexation efficacy with cyclodextrins.
  • Examination of cyclodextrin applications in solid dosage forms, parenteral, ocular, nasal, and pulmonary formulations.

Main Results:

  • Cyclodextrins form inclusion and non-inclusion complexes, as well as self-assembled aggregates, to enhance drug solubility.
  • Optimizing cyclodextrin concentration is crucial, as too much or too little can negatively impact drug bioavailability.
  • Various methods exist to enhance the intrinsic solubility of drugs and the complexation efficacy of cyclodextrins.

Conclusions:

  • Cyclodextrins are effective pharmaceutical excipients for improving drug delivery and bioavailability.
  • Understanding cyclodextrin complexation and aggregation is key to developing optimal drug formulations.
  • Cyclodextrins show promise for enhancing drug delivery via multiple administration routes, including ocular, nasal, and pulmonary.