Membrane Composition Allows the Optimization of Berberine Encapsulation in Liposomes.

Area of Science:

• Pharmacology and Drug Delivery
• Biophysics
• Materials Science

Background:

• Berberine (BBR) shows promise in combating antibiotic resistance but suffers from poor oral bioavailability.
• Liposomes are effective drug delivery systems, enhancing bioavailability and reducing side effects.
• A molecular understanding of BBR-liposome interactions is needed for rational formulation design.

Purpose of the Study:

• To rationally design liposome formulations for enhanced berberine (BBR) encapsulation and delivery.
• To identify liposome membrane compositions that maximize BBR encapsulation efficiency.
• To elucidate the molecular mechanisms governing BBR encapsulation and permeability.

Main Methods:

• Experimental screening of various liposome membrane compositions for BBR encapsulation efficiency.
• Molecular dynamics simulations to understand BBR-liposome interactions at a molecular level.
• Analysis of the influence of charged lipids and cholesterol on BBR adsorption and permeability.

Main Results:

• Encapsulation efficiency of BBR was significantly enhanced by cholesteryl hemisuccinate and cholesterol.
• Molecular dynamics simulations revealed that lipid composition modulates BBR adsorption to liposome membranes.
• Negatively charged lipids were identified as key components for maximizing BBR encapsulation.

Conclusions:

• A rational strategy for maximizing BBR liposome encapsulation using specific membrane compositions has been established.
• This work provides a foundation for designing improved BBR delivery systems to combat antibiotic resistance.
• The findings pave the way for developing more effective BBR-based therapeutics.