Poly (acrylic acid) chitosan interpolymer complexes for stomach controlled antibiotic delivery

Area of Science:

• Pharmaceutical Sciences
• Drug Delivery Systems
• Biomaterials

Background:

• Helicobacter pylori infections require effective local antibiotic therapy.
• Conventional amoxicillin delivery faces challenges with gastric degradation and short residence time.
• Developing targeted stomach-specific drug delivery systems is crucial for improving therapeutic outcomes.

Purpose of the Study:

• To develop a stomach-specific, floating hydrogel drug delivery system for amoxicillin.
• To enhance the efficacy of amoxicillin against Helicobacter pylori through improved local delivery.
• To investigate the physicochemical properties and in vivo performance of the amoxicillin-loaded polyionic complex hydrogel.

Main Methods:

• Polyionic complexes of polyacrylic acid (PAA), chitosan (CS), and amoxicillin (A) were synthesized.
• Hydrogel formulation utilized a swellable approach with a floating feature for prolonged Gastric Residence Time (GRT).
• Drug release, swelling, erosion, and stability were evaluated in simulated gastric fluid (SGF) and pH 4.0. In vivo GRT was assessed using the [13C] octanoic acid breath test in healthy volunteers.

Main Results:

• The optimized polyionic complex (PAA:CS:A 2.5:5:2) exhibited sustained amoxicillin release in enzyme-free SGF and pH 4.0.
• The hydrogel demonstrated pH-independent swelling and erosion, with maximum swelling ratios of 17.76 (SGF) and 13.42 (pH 4.0).
• The hydrogel protected amoxicillin from hydrolytic degradation and showed a prolonged GRT of up to 3 hours in vivo.

Conclusions:

• The developed amoxicillin polyionic complex hydrogel is a promising stomach-specific drug delivery system.
• The system effectively prolongs gastric residence time and protects amoxicillin, enhancing its potential for H. pylori therapy.
• This approach offers a viable strategy for improving local antibiotic treatment against gastric pathogens.