Effects of emulsifier concentration, composition, and order of addition in squalene-phosphatidylcholine oil-in-water emulsions

Pharm Dev Technol. 2011 Oct;16(5):511-9. doi: 10.3109/10837450.2010.495397. Epub 2010 Jun 16.

Abstract

Development and characterization of stable and biocompatible oil-in-water emulsions is important for improved drug and vaccine delivery. In this work, two-component emulsions consisting of squalene and phosphatidylcholine have been developed. The reproducibility of the manufacturing process is established and production efficiency is improved by altering the order of component addition. The effects of emulsifier concentration and composition on emulsion stability and biocompatibility are assessed through dynamic light scattering, zeta potential measurement, viscosity, and hemolytic activity. High concentrations of egg phosphatidylcholine emulsifier decreased initial particle size and increased initial size polydispersity. However, high emulsifier concentrations also appeared to decrease long-term emulsion stability as well as absolute zeta potential values. Substitution of naturally derived egg phosphatidylcholine with synthetic 1-palmitoyl-2-oleoyl-sn-glycero-3-phosphocholine (POPC) produced an emulsion with similar physicochemical properties and stability.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Adjuvants, Immunologic / chemistry
  • Biological Assay
  • Drug Delivery Systems
  • Emulsifying Agents / chemistry*
  • Emulsions / chemistry*
  • Humans
  • Oils / chemistry
  • Particle Size
  • Phosphatidylcholines / chemistry*
  • Reproducibility of Results
  • Squalene / chemistry*
  • Viscosity
  • Water / chemistry

Substances

  • Adjuvants, Immunologic
  • Emulsifying Agents
  • Emulsions
  • Oils
  • Phosphatidylcholines
  • Water
  • Squalene
  • 1-palmitoyl-2-oleoylphosphatidylcholine