Efficient Loading into and Controlled Release of Lipophilic Compound from Liposomes by Using Cyclodextrin as Novel...

Area of Science:

• Drug Delivery and Pharmaceutical Sciences
• Nanotechnology in Medicine
• Biochemistry

Background:

• Liposomes are key drug delivery carriers, requiring high encapsulation efficiency and controlled release for clinical use.
• Current remote loading methods using ions as trapping agents face limitations due to poor physicochemical compatibility with various drugs.
• Cyclodextrins (CDs), with their hydrophobic cavities, can form inclusion complexes with hydrophobic compounds, suggesting potential as alternative trapping agents.

Purpose of the Study:

• To evaluate sulfobutylether-β-cyclodextrin (SBE-β-CD) as a novel intraliposomal trapping agent for enhancing drug encapsulation and controlling release.
• To investigate the effect of intraliposomal SBE-β-CD on the encapsulation efficiency and release kinetics of ibuprofen (IB), a hydrophobic drug, in liposomes.

Main Methods:

• Liposomes were prepared with a pH gradient to facilitate remote drug loading.
• Sulfobutylether-β-cyclodextrin (SBE-β-CD) was incorporated into the intraliposomal aqueous phase.
• Encapsulation efficiency and in vitro drug release of ibuprofen (IB) were measured under different conditions (pH gradient alone vs. pH gradient with intraliposomal SBE-β-CD).

Main Results:

• Encapsulation efficiency of ibuprofen (IB) in liposomes with a pH gradient was approximately 27%.
• Intraliposomal SBE-β-CD significantly enhanced IB encapsulation efficiency in a concentration-dependent manner.
• SBE-β-CD inclusion suppressed the rapid early-stage release of IB, leading to more controlled drug release kinetics.

Conclusions:

• Intraliposomal SBE-β-CD acts as an effective novel trapping agent, enabling efficient encapsulation of hydrophobic drugs into liposomes.
• This SBE-β-CD-based technology facilitates controlled drug release, overcoming limitations of traditional ion-based trapping agents.
• The developed liposomal drug loading technology holds promise for improving the therapeutic benefits of various drugs compatible with cyclodextrin complexation.