The Role of Cyclodextrins in the Design and Development of Triterpene-Based Therapeutic Agents

Int J Mol Sci. 2022 Jan 10;23(2):736. doi: 10.3390/ijms23020736.

Abstract

Triterpenic compounds stand as a widely investigated class of natural compounds due to their remarkable therapeutic potential. However, their use is currently being hampered by their low solubility and, subsequently, bioavailability. In order to overcome this drawback and increase the therapeutic use of triterpenes, cyclodextrins have been introduced as water solubility enhancers; cyclodextrins are starch derivatives that possess hydrophobic internal cavities that can incorporate lipophilic molecules and exterior surfaces that can be subjected to various derivatizations in order to improve their biological behavior. This review aims to summarize the most recent achievements in terms of triterpene:cyclodextrin inclusion complexes and bioconjugates, emphasizing their practical applications including the development of new isolation and bioproduction protocols, the elucidation of their underlying mechanism of action, the optimization of triterpenes' therapeutic effects and the development of new topical formulations.

Keywords: cyclodextrins; cytotoxicity; inclusion complexes; phytocompounds; triterpenes.

Publication types

  • Review

MeSH terms

  • Chemical Phenomena
  • Cyclodextrins / chemistry*
  • Cyclodextrins / classification
  • Drug Compounding
  • Drug Design*
  • Drug Development*
  • Humans
  • Molecular Structure
  • Plant Extracts / chemistry
  • Plant Extracts / isolation & purification
  • Plant Extracts / pharmacology
  • Structure-Activity Relationship
  • Triterpenes / chemistry*
  • Triterpenes / isolation & purification
  • Triterpenes / pharmacology*

Substances

  • Cyclodextrins
  • Plant Extracts
  • Triterpenes