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Enhanced Antimicrobial Action of Chlorhexidine Loaded in Shellac Nanoparticles with Cationic Surface Functionality.

Saba S M Al-Obaidy1,2, Gillian M Greenway1, Vesselin N Paunov3

  • 1Department of Chemistry and Biochemistry, University of Hull, Hull HU6 7RX, UK.

Pharmaceutics
|September 28, 2021
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Summary

We developed dual-functionalized shellac nanoparticles (NPs) that significantly boost chlorhexidine (CHX) antimicrobial activity. This novel nanocarrier system enhances CHX efficacy against oral pathogens, potentially reducing required concentrations for treating infections.

Keywords:
E. coliODTABPoloxamer 407antimicrobial nanocarrierschlorhexidinemicroalgaenanoparticlesshellacyeast

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Area of Science:

  • Nanotechnology
  • Materials Science
  • Antimicrobial Agents

Background:

  • Chlorhexidine (CHX) is a widely used antiseptic, but its efficacy can be limited by formulation and delivery.
  • Nanoparticle-based drug delivery systems offer potential for enhanced antimicrobial action.
  • Shellac nanoparticles (NPs) provide a biocompatible platform for drug encapsulation.

Purpose of the Study:

  • To develop and characterize an active nanocarrier for chlorhexidine (CHX) using dual surface-functionalized shellac NPs.
  • To investigate the encapsulation efficiency, release kinetics, and antimicrobial activity of the novel CHX nanocarrier.
  • To explore the impact of dual functionalization on CHX's antimicrobial enhancement.

Main Methods:

  • Fabrication of CHX-loaded shellac NPs via pH-induced co-precipitation with Poloxamer 407 (P407) stabilization.
  • Surface modification of NPs with octadecyl trimethyl ammonium bromide (ODTAB) to impart cationic functionality.
  • Assessment of CHX encapsulation efficiency and release kinetics.
  • Evaluation of antimicrobial activity against *E. coli*, *S. cerevisiae*, and *C. reinhardtii*.

Main Results:

  • Dual surface functionalization of shellac NPs with ODTAB significantly amplified the antimicrobial action of CHX.
  • Non-coated, CHX-loaded NPs showed inferior activity compared to free CHX due to negative surface charge.
  • The enhanced activity is attributed to increased electrostatic adhesion between cationic NPs and anionic microbial cell walls, enabling targeted CHX delivery.
  • Tested microorganisms included *E. coli* (Gram-negative bacterium), *S. cerevisiae* (yeast), and *C. reinhardtii* (microalgae).

Conclusions:

  • Dual surface-functionalized shellac nanoparticles represent an effective nanocarrier for enhancing chlorhexidine's antimicrobial efficacy.
  • The cationic surface charge is crucial for improved antimicrobial performance through enhanced cellular adhesion and targeted drug delivery.
  • This novel nanocarrier system holds promise for developing advanced dental formulations to combat oral infections like gingivitis and periodontitis with potentially lower CHX concentrations.