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Statistical Optimization of Oral Vancomycin-Eudragit RS Nanoparticles Using Response Surface Methodology.

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Optimized vancomycin (VCM) nanoparticles using Eudragit RS via double emulsion improved physicochemical properties for oral delivery. The formulation achieved high encapsulation efficiency and controlled drug release over 24 hours.

Keywords:
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Area of Science:

  • Pharmaceutical Sciences
  • Materials Science

Background:

  • Vancomycin (VCM) is a critical antibiotic often administered intravenously.
  • Developing oral VCM formulations faces challenges due to poor bioavailability and stability.
  • Eudragit polymers offer potential for controlled drug release systems.

Purpose of the Study:

  • To optimize Eudragit-based vancomycin (VCM) nanoparticles for enhanced oral administration.
  • To investigate the impact of formulation variables on nanoparticle physicochemical properties.
  • To evaluate the in vitro drug release profile and kinetics.

Main Methods:

  • Preparation of VCM nanoparticles using a W1/O/W2 double-emulsion solvent evaporation method with Eudragit RS.
  • Optimization using a Box-Behnken design to study independent variables (RPM, emulsifier concentration, etc.) on dependent variables (yield, encapsulation efficiency, particle size).
  • Characterization of nanoparticles including zeta potential and in vitro release studies fitted to kinetic models.

Main Results:

  • Optimal VCM nanoparticle formulation achieved at a 1:2 drug to polymer ratio, 0.2% emulsifier, 25 mL organic phase, 25 mL aqueous phase, 3 min stirring, and 26000 RPM.
  • High drug loading (R2 = 90.82) was influenced by RPM and emulsifier concentration.
  • Highest entrapment efficiency observed at a 1:3 drug to polymer ratio; nanoparticles exhibited a positive zeta potential.
  • In vitro release showed an initial burst followed by slow release over 24 hours, consistent with diffusion-controlled release (Peppas model).

Conclusions:

  • Optimized Eudragit VCM nanoparticles demonstrate favorable physicochemical properties for oral delivery.
  • The formulation exhibits controlled release characteristics, potentially improving VCM therapeutic efficacy.
  • The study provides a robust method for developing Eudragit-based nanoparticles for oral antibiotic administration.