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Related Experiment Videos

Temperature and pH-sensitive polymers for human calcitonin delivery

A Serres1, M Baudys, S W Kim

  • 1University of Utah, Department of Pharmaceutics and Pharmaceutical Chemistry, Center for Controlled Chemical Delivery, Salt Lake City 84112, USA.

Pharmaceutical Research
|February 1, 1996
PubMed
Summary

New polymeric beads effectively deliver calcitonin orally. Higher acrylic acid content in stimuli-sensitive polymers improves peptide loading, stability, and release for enhanced drug delivery.

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Area of Science:

  • Biomaterials Science
  • Polymer Chemistry
  • Drug Delivery Systems

Background:

  • Stimuli-sensitive polymers offer potential for oral peptide drug delivery.
  • They protect peptide drugs from gastric degradation and enable controlled release.
  • Calcitonin is a peptide drug suitable for this delivery approach.

Purpose of the Study:

  • To fabricate polymeric beads using pH/temperature-sensitive terpolymers.
  • To load the beads with human calcitonin for oral delivery.
  • To investigate the influence of polymer composition and loading conditions on drug encapsulation and release.

Main Methods:

  • Polymeric beads were formed by dropwise addition of a polymer-drug solution into an oil bath above the polymer's Lower Critical Solution Temperature (LCST).

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  • Human calcitonin loading, stability, and release were analyzed using High-Performance Liquid Chromatography (HPLC), Circular Dichroism (CD), and Fourier-Transform Infrared Spectroscopy (FTIR).
  • In vivo studies assessed the biological activity of the released calcitonin.

    • Main Results:

    • Optimal loading conditions were identified as a 20 mM glycine/HCl buffer (pH 3.0) with 0.15 M NaCl and an oil bath temperature of 23°C.
    • Increasing acrylic acid content in the terpolymers from 0 to 10 mol% significantly enhanced calcitonin loading efficiency, stability, and release.
    • The in vivo biological activity of the released human calcitonin was successfully preserved.

    Conclusions:

    • Polymeric beads with higher acrylic acid content demonstrate superior loading, stability, and release of human calcitonin.
    • These developed beads represent a promising new system for the oral delivery of calcitonin and other peptide drugs.