Solid-state nanoparticle coated emulsions for encapsulation and improving the chemical stability of all-trans-retinol

Int J Pharm. 2012 Feb 28;423(2):384-91. doi: 10.1016/j.ijpharm.2011.12.027. Epub 2011 Dec 23.

Abstract

Submicron oil-in-water (o/w) emulsions stabilised with conventional surfactants and silica nanoparticles were prepared and freeze-dried to obtain free-flowing powders with good redispersibility and a three-dimensional porous matrix structure. Solid-state emulsions were characterised for visual appearance, particle size distribution, zeta potential and reconstitution properties after freeze-drying with various sugars and at a range of sugar to oil ratios. Comparative degradation kinetics of all-trans-retinol from freeze-dried and liquid emulsions was investigated as a function of storage temperatures. Optimum stability was observed for silica-coated oleylamine emulsions at 4 °C in their wet state. The half-life of all-trans-retinol was 25.66 and 22.08 weeks for silica incorporation from the oil and water phases respectively. This was ∼4 times higher compared to the equivalent solid-state emulsions with drug half-life of 6.18 and 6.06 weeks at 4 °C. Exceptionally, at a storage temperature of 40 °C, the chemical stability of the drug was 3 times higher in the solid-state compared to the wet emulsions which confirmed that freeze-drying is a promising approach to improve the chemical stability of water-labile compounds provided that the storage conditions are optimised.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Chemistry, Pharmaceutical
  • Drug Compounding
  • Drug Stability
  • Drug Storage
  • Emulsions
  • Freeze Drying
  • Half-Life
  • Kinetics
  • Nanoparticles*
  • Nanotechnology*
  • Oils / chemistry
  • Particle Size
  • Powders
  • Silicon Dioxide / chemistry*
  • Surface-Active Agents / chemistry
  • Technology, Pharmaceutical / methods*
  • Temperature
  • Vitamin A / chemistry*
  • Vitamins / chemistry*

Substances

  • Emulsions
  • Oils
  • Powders
  • Surface-Active Agents
  • Vitamins
  • Vitamin A
  • Silicon Dioxide