Cyclodextrins--enabling excipients: their present and future use in pharmaceuticals

Area of Science:

• Pharmaceutical Science
• Drug Delivery Systems
• Supramolecular Chemistry

Background:

• Cyclodextrins (CDs) are crucial excipients for complexing hydrophobic drugs.
• CD complexation improves drug aqueous solubility and stability.
• This facilitates the development of advanced formulations for poorly soluble compounds.

Purpose of the Study:

• To review the structural features of available cyclodextrins.
• To discuss their impact on drug complexation performance.
• To summarize quality, production, safety, and regulatory aspects.

Main Methods:

• Evaluation of structural characteristics of alpha-, beta-, and gamma-CD and their derivatives (M-, HP-, SBE-beta-CD).
• Analysis of complexation performance based on structural features.
• Review of quality control, production standards, and safety data.
• Summary of global regulatory landscapes for cyclodextrins.

Main Results:

• Ten pharmaceutical products currently utilize CD formulations.
• Specific structural attributes influence the complexation efficiency of different CDs.
• Optimal specifications for production and quality are presented for key CDs.
• Regulatory status in Japan, US, and Europe is detailed.

Conclusions:

• Cyclodextrins offer versatile solutions for formulating challenging hydrophobic drugs.
• Understanding CD structure-property relationships is key for optimal formulation design.
• Comprehensive quality and safety data support their pharmaceutical use.
• Regulatory insights are provided for global market access.