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Formulation optimization of chelerythrine loaded O-carboxymethylchitosan microspheres using response surface

Gui-yin Li1, Ming Zhong, Zhi-de Zhou

  • 1School of Life and Environmental Sciences, Guilin University of Electronic Technology, Guilin, Guangxi 541014, China.

International Journal of Biological Macromolecules
|September 6, 2011
PubMed
Summary

This study developed optimized chelerythrine (CHE) loaded O-carboxymethylchitosan (O-CMCS) microspheres using response surface methodology. The optimized formulation demonstrated controlled release, showing potential for drug delivery applications.

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Area of Science:

  • Materials Science
  • Pharmaceutical Sciences
  • Chemical Engineering

Background:

  • O-carboxymethylchitosan (O-CMCS) is a promising biomaterial for drug delivery.
  • Chelerythrine (CHE) is a bioactive alkaloid with therapeutic potential.
  • Developing efficient drug delivery systems for CHE is crucial for its clinical application.

Purpose of the Study:

  • To develop and optimize O-carboxymethylchitosan (O-CMCS) microspheres loaded with chelerythrine (CHE) using emulsion cross-linking.
  • To optimize process and formulation variables for maximum drug loading and encapsulation efficiency.
  • To characterize the optimized microspheres for particle size, morphology, and in vitro drug release.

Main Methods:

  • Emulsion cross-linking method for microsphere preparation.
  • Response Surface Methodology (RSM) with Box-Behnken Design (BBD) for optimization.
  • Desirability function for achieving maximum drug loading and encapsulation efficiency.
  • Characterization of microspheres including particle size, morphology, and in vitro drug release studies.

Main Results:

  • Optimized O-CMCS/CHE microspheres were successfully prepared.
  • Mathematical models were developed to correlate independent variables (O-CMCS/CHE ratio, O/W phase ratio, O-CMCS concentration) with dependent variables (drug loading, encapsulation efficiency).
  • Optimized microspheres exhibited a mean particle size of 12.18 μm, drug loading of 4.16 ± 3.36%, encapsulation efficiency of 57.40 ± 2.30%, and 54.5% in vitro drug release at pH 7.4 after 70 hours.

Conclusions:

  • The combination of RSM, BBD, and desirability function effectively optimized the O-CMCS microsphere formulation for CHE delivery.
  • O-carboxymethylchitosan (O-CMCS) shows significant potential as a controlled drug delivery carrier.
  • The developed method provides a viable approach for lab-scale microemulsion process development for drug delivery systems.