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Related Experiment Videos

pH and osmotic pressure inside biodegradable microspheres during erosion.

A Brunner1, K Mäder, A Göpferich

  • 1Aventis Research & Technologies, Industriepark Hoechst, Frankfurt am Main, Germany.

Pharmaceutical Research
|July 9, 1999
PubMed
Summary

Researchers measured pH and osmotic pressure in biodegradable microspheres. Poly(lactic acid) microspheres showed increased osmotic pressure, while poly(lactic-co-glycolic acid) microspheres maintained an acidic pH, crucial for drug stability.

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Area of Science:

  • Biomaterials Science
  • Polymer Chemistry
  • Drug Delivery Systems

Background:

  • Biodegradable microspheres are widely used for controlled drug delivery.
  • Understanding the internal microenvironment (pH, osmotic pressure) is critical for predicting drug stability and release kinetics.
  • Polymers like poly(lactic acid) (PLA) and poly(lactic-co-glycolic acid) (PLGA) are common materials for microsphere fabrication.

Purpose of the Study:

  • To quantify changes in pH and osmotic pressure within the aqueous compartments of PLA and PLGA biodegradable microspheres during their degradation.
  • To assess the influence of formulation components on the internal pH of PLGA microspheres.

Main Methods:

  • Internal osmotic pressure in PLA microspheres was determined using differential scanning calorimetry (DSC) by analyzing the melting point depression of the aqueous phase.

Related Experiment Videos

  • Internal pH of PLGA microspheres was measured using electron paramagnetic resonance (EPR) spectroscopy with a pH-sensitive spin probe.

    • Main Results:

    • Osmotic pressure within PLA microspheres increased to approximately 600 mOsm within four days, then decreased to 400 mOsm after two weeks.
    • The internal pH of PLGA microspheres was measured to be less than or equal to 4.7.
    • Addition of basic drugs (e.g., gentamicin free base) or buffering agents increased the pH, but it did not exceed 6 within 13 hours.

    Conclusions:

    • Differential scanning calorimetry (DSC) and electron paramagnetic resonance (EPR) are effective techniques for characterizing the internal chemical microenvironment of eroding microspheres.
    • This characterization provides valuable data for predicting the stability of sensitive compounds, such as peptides and proteins, encapsulated within biodegradable polymers.
    • Future research combining this microenvironmental data with drug stability information can optimize drug delivery system design.