Effect of squalane on mebendazole-loaded Compritol® nanoparticles

J Biomater Sci Polym Ed. 2015;26(13):868-80. doi: 10.1080/09205063.2015.1061351. Epub 2015 Jul 9.

Abstract

The objective of this study is to develop nanostructured lipid formulations of Compritol for the delivery of mebendazole. The formulations were prepared with Compritol 888 ATO, squalane, and Pluronic F68. Nine batches with different amounts of modifier, squalane, and drug were prepared. The formulations were characterized by evaluating particle size, morphology, and zeta potential. The thermal properties of the formulations were analyzed by differential scanning calorimetry (DSC). The encapsulation efficiency of each formulation and the drug release rates from each formulation were quantified by UPLC. The particles were spherical and had median particle sizes between 300 and 600 nm (50th percentile). A linear relationship was observed between Compritol/squalane composition and the melting point of the mixture. The DSC scans of the formulations revealed some recrystallization of the drug from the formulations, and the amount of recrystallization correlated with the amount of squalane in the formulation. Approximately, 70% efficiency of encapsulation was observed in the formulations with 30% (w/w) squalane, and these formulations also had faster dissolution rates compared to the other formulations. Overall, the formulations with 30% squalane are the preferred formulation for future testing.

Keywords: Compritol; NLC; NLF; mebendazole; nanostructured lipid; squalane.

Publication types

  • Research Support, N.I.H., Extramural
  • Research Support, Non-U.S. Gov't

MeSH terms

  • Calorimetry, Differential Scanning
  • Drug Carriers* / chemistry
  • Drug Liberation
  • Fatty Acids* / chemistry
  • Mebendazole / administration & dosage*
  • Mebendazole / pharmacokinetics
  • Microscopy, Electron, Scanning
  • Nanoparticles* / chemistry
  • Particle Size
  • Poloxamer / chemistry
  • Squalene / analogs & derivatives*
  • Squalene / chemistry
  • Transition Temperature
  • Tubulin Modulators / administration & dosage*
  • Tubulin Modulators / pharmacokinetics

Substances

  • Drug Carriers
  • Fatty Acids
  • Tubulin Modulators
  • Poloxamer
  • glyceryl behenate
  • Squalene
  • Mebendazole
  • squalane