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Do surface active parenteral formulations cause inflammation?

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Area of Science:

  • Pharmacology
  • Biophysics

Background:

  • Parenteral formulations can cause local irritation and inflammation.
  • Biological effects of interfacial activity are less understood than pH or osmolality.
  • Interfacial activity is a key physico-chemical parameter influencing drug safety.

Purpose of the Study:

  • To measure interfacial activity in various biological and pharmaceutical systems.
  • To correlate interfacial activity with known biological effects of substances.
  • To test the hypothesis that interfacial activity predicts in vivo biological responses.

Main Methods:

  • Measured interfacial pressure in systems including human plasma, amphiphiles, anesthetics, and antibiotics.
  • Calculated relative interfacial pressure for 50% maximal effect.
  • Compared measured interfacial activity with reported in vivo biological effects.

Main Results:

  • Highest interfacial activity observed in triglyceride/plasma systems.
  • Erythromycin and dicloxacillin showed the highest interfacial activity among tested antibiotics.
  • Severe biological effects correlated with relative interfacial activity above 35-45%.

Conclusions:

  • Interfacial activity is a significant factor in parenteral formulation-induced tissue damage and inflammation.
  • Quantifying interfacial activity can predict potential adverse biological effects.
  • Understanding interfacial activity is crucial for developing safer parenteral drugs.