Multifunctional erythromycin-loaded liposomes: a methodological optimization for enhanced mucoadhesion, antioxidant...

Area of Science:

• Nanotechnology
• Materials Science
• Pharmacology

Background:

• Liposomes are advanced nanocarriers for antibacterial agents, improving drug pharmacokinetics to combat antibiotic resistance.
• Erythromycin (ERY) is a key antibiotic, but its delivery can be enhanced for better efficacy.
• Chitosan oligomers (CSO) offer mucoadhesive, antioxidant, and antimicrobial properties beneficial for drug delivery systems.

Purpose of the Study:

• To systematically optimize erythromycin-loaded liposomes (ERY-liposomes) coated with chitosan oligomers (CSO).
• To achieve nanoscale drug encapsulation with enhanced mucoadhesive, antioxidant, antimicrobial, and biocompatibility attributes.
• To evaluate the physicochemical, structural, release, and biological properties of the optimized ERY-liposomes.

Main Methods:

• Multivariate analysis was used to optimize critical formulation parameters (lipid-to-drug ratio, film formation, hydration, downsizing, CSO properties, cryoprotectant).
• Comprehensive physicochemical and structural characterization using FTIR, 1H-NMR, DLS, STEM, AFM, XRD, and POM.
• In vitro assessment of drug release kinetics, antibacterial activity, antioxidant capacity, mucoadhesion, and cytocompatibility.

Main Results:

• Optimized ERY-liposomes exhibited 63% encapsulation efficiency, 97 nm size, and low PDI (<0.1).
• Structural analysis confirmed drug incorporation in an amorphous state within densely packed vesicles with a rough CSO coating.
• Formulation showed sustained ERY release, potent 24-hour antibacterial activity, significant antioxidant effects (80% radical inhibition), mucoadhesion, and fibroblast cytocompatibility.

Conclusions:

• The optimized ERY-liposomes demonstrate significant potential as advanced nanocarriers for erythromycin delivery.
• The formulation combines enhanced drug encapsulation, controlled release, potent antimicrobial action, and beneficial biological properties.
• These findings support the therapeutic application of ERY-liposomes in addressing bacterial infections and antibiotic resistance.