Evaluation of the digestibility of solid lipid nanoparticles of glyceryl dibehenate produced by two techniques: Ultrasonication and spray-flash evaporation

Eur J Pharm Sci. 2018 Jan 1:111:91-95. doi: 10.1016/j.ejps.2017.09.049. Epub 2017 Sep 29.

Abstract

Objective: To evaluate the digestibility of Solid Lipid Nanoparticles (SLN) of glyceryl dibehenate prepared either with surfactants by ultrasonication or without surfactant by spray-flash evaporation.

Methods: SLN of glyceryl dibehenate (Compritol® 888 ATO) were produced by two processes: (i) high-shear homogenization with a solution of water-soluble surfactants followed by ultrasonication (ii) and Spray-Flash Evaporation (SFE) of the pure lipid. The digestibility of these nanoparticles was then tested by in vitro lipolysis using a pH-stat apparatus and the assay of glycerides by gel phase chromatography.

Results: SLN of glyceryl dibehenate prepared by ultrasonication exhibited a mean particle size of 180nm and showed a limited digestion of the lipid excipient. SLN comprising only glyceryl dibehenate produced by SFE have a mean particle size between 235 and 411nm depending on process parameters. These nanoparticles were not digested by lipases. The presence of surfactant at the lipid/water interface of the SLN seems to be mandatory to allow the adsorption of the lipase and degradation of glyceryl behenate.

Conclusions: Glyceryl dibehenate as a solid particle - even as a SLN - is not digested by pancreatin during in vitro lipolysis test.

Keywords: Glyceryl dibehenate; Lipolysis; SLN; Spray-flash evaporation; Ultrasonication.

MeSH terms

  • Chemistry, Pharmaceutical
  • Digestion
  • Excipients / chemistry*
  • Fatty Acids / chemistry*
  • Lipolysis
  • Models, Biological
  • Nanoparticles / chemistry*
  • Pancreatin / chemistry
  • Particle Size
  • Sonication
  • Surface-Active Agents / chemistry*
  • Technology, Pharmaceutical / methods*

Substances

  • Excipients
  • Fatty Acids
  • Surface-Active Agents
  • glyceryl behenate
  • Pancreatin