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"Micro to macro (M2M)"--A novel approach for intravenous delivery of propofol

Robert Damitz1, Anuj Chauhan1

  • 1Department of Chemical Engineering, University of Florida, Gainesville, FL 32611, USA.

International Journal of Pharmaceutics
|August 12, 2015
PubMed
Abstract

Insights

A novel micro to macro (M2M) approach transforms propofol microemulsions into macroemulsions just before injection. This method enhances stability, manufacturability, and may reduce injection pain for anesthetic drugs.

Area of Science:

  • Pharmaceutical Sciences
  • Materials Science
  • Chemical Engineering

Background:

  • Propofol emulsions face challenges with limited shelf life and injection site pain.
  • Microemulsions offer improved stability and simpler manufacturing but can increase injection discomfort.

Purpose of the Study:

  • To introduce and validate a novel micro to macro (M2M) approach for propofol formulations.
  • To destabilize propofol microemulsions into macroemulsions immediately prior to administration.

Main Methods:

  • Preparation of propofol microemulsions at high drug loadings.
  • Determination of compositions that destabilize into macroemulsions upon aqueous dilution.
  • Measurement of droplet growth using dynamic light scattering and turbidity.
  • Analysis of experimental data using a coalescence model.

Main Results:

  • Dilution-induced destabilization of microemulsions into macroemulsions occurs rapidly (seconds to minutes).
  • Resulting macroemulsions are metastable with droplet sizes around 1 micron, stable for hours.
  • Coalescence model accurately predicts droplet growth kinetics with adjusted parameters.

Conclusions:

  • The M2M approach is feasible for propofol, potentially improving drug product stability and reducing injection pain.
  • This strategy may be applicable to other hydrophobic vesicant drugs, enhancing formulation options.
Keywords:
CoalescenceFormulationInterfacial phenomenaMicroemulsionPropofolSurfactant

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