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β-Cyclodextrins as a Solubilization Tool for Insoluble APIs

December 16th 2015

This White Paper demonstrates why β-Cyclodextrins (β-CDs) are the best solution for improving solubility of poorly soluble active pharmaceutical ingredients (APIs).



The use of β-CDs can help to overcome one of the main challenges in drug delivery: guaranteeing the bioavailability of APIs, especially when they are poorly soluble and/or with a limited gastrointestinal permeability.

To improve aqueous solubility and thus the therapeutic effectiveness of such compounds, a number of formulation strategies have already been largely tested. It is a big challenge to find the right solubilization tool for these active ingredients.


The paper explains why to choose β-CDs as a solubilization tool, and how to successfully complexate active ingredients.
It includes illustrative case studies to ease the understanding of the tools used to study inclusion on β-CDs: phase solubility, stability constant, and complexation efficiency, complexation processes in liquid and solid state. These studies focus on highly permeable drugs with limited water solubility, considered as “BCS class II”: Zotepine and Zaleplon.


The White Paper shows that β-CDs can be used to increase aqueous solubility of APIs as well as their chemical and physical stability.

β-CDs can also:

  • Reduce toxicity (e.g.: local irritation after topical or oral administration)
  • Enhance drug delivery to and through biological membranes
  • Mask bad taste or odor
  • Convert liquid drugs to amorphous powders


These studies demonstrate that KLEPTOSE® (Roquette’s range of chemically modified β-CDs) are fully adapted tools to increase the aqueous solubility of APIs.

The patent situation has evolved, in favour of more uses of HPβ-CDs. This new context makes this excipient an easily accessible formulation aid for the development scientist.


Supplier Information
Supplier: Roquette Pharma
Address: 62080 Lestrem, France
Tel: +33 3 21 63 36 00
Fax: +33 3 21 63 94 64

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