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February 5, 2026Journal of Biomaterials Science Polymer Edition0 citations

Formulation and evaluation of azithromycin loaded chitosan nanoparticles for its antibiofilm activity

CRChandana R.HAH. M. ASHVINIAl-Ameen College of Pharmacy

Key Points

This research aims to formulate and evaluate azithromycin-loaded chitosan nanoparticles for improved antimicrobial and antibiofilm efficacy.
Formulated nanoparticles by ionic gelation using chitosan and TPP.
Coated nanoparticles with PAA and cross-linked using EDC.
Characterized nanoparticles using FTIR, DSC, and electron microscopy techniques.
Conducted in-vitro drug release studies over 24 hours.
Assessed antimicrobial activity through zone of inhibition measurements against Staphylococcus aureus.
Optimized formulation exhibited a particle size of 287.3 nm and high entrapment efficiency of 98.35%.
In-vitro drug release showed sustained release of 90% over 24 hours.
Demonstrated enhanced antimicrobial activity with a zone of inhibition of 17-21 mm against Staphylococcus aureus.
Achieved 71% inhibition of biofilm biomass and a reduction of extracellular polymeric substances (EPS) by 40 µg/mL.

Abstract

The present study focused on the formulation and evaluation of azithromycin-loaded chitosan nanoparticles (AZM-CSNPs) to enhance antimicrobial and antibiofilm efficacy. The nanoparticles were prepared by ionic gelation of chitosan with TPP, followed by PAA coating and covalent conjugation using EDC cross-linking to obtain stable CTS/TPP-PAA NPs. Preformulation studies (FTIR and DSC) confirmed drug-polymer compatibility, while physicochemical characterization revealed that the optimized formulation (CNP 1) exhibited a particle size of 287.3 nm, PDI of 0.352, zeta potential of -22.0 mV, and entrapment efficiency of 98.35%. Transmission Electron Microscopy and Scanning Electron Microscopy analyses confirmed spherical, uniformly distributed nanoparticles. In-vitro drug release demonstrated sustained release of 90% over 24 h. The formulation showed enhanced antimicrobial activity against Staphylococcus aureus with a zone of inhibition of 17-21 mm and significant antibiofilm activity, evidenced by 71% biofilm biomass inhibition and 40 µg/mL EPS reduction. Overall, AZM-CSNPs displayed superior performance compared to pure azithromycin, suggesting their potential as an effective nanocarrier system for treating biofilm-associated infections and addressing antibiotic resistance.

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