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Remote loading of curcumin-in-modified β-cyclodextrins into liposomes using a transmembrane pH gradient.

Fadwa Odeh1, Hamdi Nsairat1, Walhan Alshaer2

  • 1Department of Chemistry, The University of Jordan Amman 11942 Jordan f.odeh@ju.edu.jo +962 6 5355000 ext. 22152 +962 792950409.

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This study introduces a novel method for enhancing curcumin (CRM) delivery using modified cyclodextrins and liposomes. This approach significantly improves CRM encapsulation efficiency, overcoming solubility limitations for potential therapeutic applications.

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Area of Science:

  • Pharmaceutical Nanotechnology
  • Drug Delivery Systems
  • Biochemistry

Background:

  • Curcumin (CRM) possesses significant therapeutic potential due to its antioxidative, anti-inflammatory, and anticancer properties.
  • Low water solubility and poor bioavailability limit the clinical application of curcumin.
  • Intraliposomal remote loading is an effective strategy for encapsulating drugs within liposomes using a pH gradient.

Purpose of the Study:

  • To develop a novel method for the remote loading of curcumin into liposomes.
  • To utilize chemically modified beta-cyclodextrins (βCDs) as carriers and solubilizers for curcumin.
  • To enhance the encapsulation efficiency of curcumin within liposomes.

Main Methods:

  • Preparation of amino-modified β-cyclodextrins (E-βCD and D-βCD).
  • Formation of curcumin-βCD inclusion complexes via solvent evaporation.
  • Active loading of curcumin-βCD complexes into liposomes using a pH gradient.

Main Results:

  • Characterization confirmed the formation of curcumin-βCD inclusion complexes with determined stoichiometric ratios and formation constants.
  • Liposome characterization confirmed a homogeneous population before and after active loading.
  • Encapsulation efficiencies for curcumin-βCD complexes into liposomes were significantly increased (up to 51.1%), representing a >5-fold improvement over conventional liposomes.

Conclusions:

  • Chemically modified β-cyclodextrins enable effective remote loading of curcumin into liposomes.
  • This novel approach significantly enhances curcumin encapsulation efficiency, addressing its poor solubility and bioavailability.
  • The developed method offers a promising strategy for incorporating hydrophobic drugs into liposomes for improved therapeutic delivery.