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Related Experiment Videos

Release behavior of bioactive agents from pH-sensitive hydrogels

A R Khare1, N A Peppas

  • 1School of Chemical Engineering, Purdue University, West Lafayette, IN 47907-1283.

Journal of Biomaterials Science. Polymer Edition
|January 1, 1993
PubMed
Summary

pH-sensitive anionic copolymers were used to create controlled drug delivery systems for theophylline, proxyphylline, and oxprenolol hydrochloride. Drug release rates and mechanisms depend on pH, ionic strength, and polymer ionization, showing non-Fickian release behavior.

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Area of Science:

  • Polymer chemistry
  • Materials science
  • Pharmaceutical sciences

Background:

  • Controlled drug delivery systems aim to modulate therapeutic agent release profiles.
  • Anionic copolymers offer potential for pH-sensitive drug release applications.

Purpose of the Study:

  • To prepare and characterize controlled release systems for theophylline, proxyphylline, and oxprenolol hydrochloride.
  • To investigate the influence of pH, ionic strength, and polymer ionization on drug release kinetics and mechanisms.

Main Methods:

  • Synthesis of pH-sensitive anionic copolymers of 2-hydroxyethyl methacrylate with acrylic acid or methacrylic acid.
  • Preparation of controlled release formulations incorporating theophylline, proxyphylline, and oxprenolol hydrochloride.
  • In vitro drug release studies conducted in simulated biological fluids at varying pH and ionic strength.

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Main Results:

  • Drug release rates and mechanisms were significantly influenced by buffer pH, ionic strength, and salt composition.
  • Calculated drug diffusion coefficients were on the order of 10(-7) cm2/s and correlated with the degree of polymer swelling.
  • Non-Fickian drug release kinetics were observed across all tested dissolution media.
  • Non-ionized polymer networks exhibited the lowest drug release rates, consistent with ionization-swelling-release relationships.

Conclusions:

  • pH-sensitive anionic copolymers can effectively modulate the release of theophylline, proxyphylline, and oxprenolol hydrochloride.
  • Polymer ionization, swelling, pH, and ionic strength are critical factors governing drug release kinetics and mechanisms.
  • These findings support the development of tailored polymer-drug formulations for optimized therapeutic outcomes.