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

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.