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Ophthalmic drug delivery faces major limitations due to poor absorption across the corneal membrane. This process is primarily driven by diffusion and is influenced by two main factors: the physicochemical properties of the drug and tear drainage. Most ophthalmic drugs, such as pilocarpine, epinephrine, atropine, and local anesthetics, are weak bases. They are typically formulated at an acidic pH to enhance chemical stability. However, this leads to high ionization, reducing their ability to...
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On formulating ophthalmic emulsions.

Roozbeh Mafi1, Cameron Gray1, Robert Pelton1

  • 1Department of Chemical Engineering, McMaster University, Hamilton, ON L8S 4L7, Canada.

Colloids and Surfaces. B, Biointerfaces
|July 14, 2014
PubMed
Summary
This summary is machine-generated.

Formulating stable eye drops is difficult due to polymer-induced aggregation. This study found that higher polymer molecular weight lowers the critical flocculation concentration (CFC), enabling better ophthalmic emulsion design.

Keywords:
Depletion flocculationEmulsion stabilityEye drop formulationGuarOverlap concentration

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Area of Science:

  • Pharmaceutical Sciences
  • Colloid and Surface Chemistry
  • Polymer Science

Background:

  • Ophthalmic emulsions (eye drops) require stability for long shelf lives.
  • Water-soluble polymers enhance eye drop function but can cause lipid and drug aggregation.
  • Aggregation occurs above the critical flocculation concentration (CFC).

Purpose of the Study:

  • To develop a predictive method for the critical flocculation concentration (CFC) of polymers in ophthalmic emulsions.
  • To establish a design rule for stable ophthalmic emulsion formulations.

Main Methods:

  • Hydrolysis of high molecular weight guar to create samples with varying molecular weights.
  • Measurement of CFC and critical viscosity concentration using electrophoresis, dynamic light scattering, and rheology.
  • Correlation of CFC with polymer molecular weight and overlap concentration.

Main Results:

  • A higher guar molecular weight resulted in a lower CFC.
  • Guar CFC values approximated the polymer overlap concentration in solution.
  • The study proposes CFC can be estimated using polymer molecular weight and Mark-Houwink parameters.

Conclusions:

  • The molecular weight of water-soluble polymers is a key factor in determining the critical flocculation concentration (CFC).
  • A predictive model for CFC based on readily available polymer parameters can guide the formulation of stable ophthalmic emulsions.
  • This research offers a design rule for creating long-lasting, transparent eye drops.