Preparation, optimization, and in-vitro characterization of α-tocopherol-loaded solid lipid nanoparticles (SLNs)

Drug Dev Ind Pharm. 2020 Jan;46(1):159-171. doi: 10.1080/03639045.2019.1711388. Epub 2020 Jan 13.

Abstract

Objective: The main scope of present investigation was preparation and physicochemical characterization of solid lipid nanoparticles (SLNs) loaded by α-tocopherol acetate (ATA).Methods: ATA-loaded nanoparticles were prepared by solvent injection-homogenization technique using stearic acid as the solid lipid, phosphatidylcholine as the stabilizer and finally coated by chitosan with the aim of increasing z-potential and also having a more stable nano-formulation. Then, characterization of SLNs has been conducted using dynamic light scattering (DLS), zeta potential measurement, Fourier transform infrared spectroscopy (FTIR), and differential scanning calorimetry (DSC).Results: Nanoparticles with average sizes of 175 ± 15 nm and zeta potential of +35 ± 2.5 mV were obtained. An excellent drug entrapment efficiency of 90.58 ± 1.38% was obtained with a no-burst slow release up to about 10 days tested. The final plateau of release of ATA from nanoparticulate system within 216 h was 61.13 ± 0.13% which was approached in about 150 h. Physical stability studies showed that the ATA nano-formulation remained stable with slight increase in mean particle size and polydispersity index over a 3-month period in refrigerated temperature. Considering both FTIR and DSC analysis, it can be concluded that there is no new band formation between materials and ATA in our nano-formulation. Particle sizes obtained using AFM images are in a good agreement to those established from the DLS analysis.Conclusion: These data showed a promising delivery system for vitamin E based on SLN platform.

Keywords: Solid lipid nanoparticles (SLNs); drug delivery; solvent injection-homogenization technique; vitamin E; α-tocopherol acetate.

MeSH terms

  • Chemistry, Pharmaceutical
  • Chitosan / chemistry
  • Delayed-Action Preparations
  • Drug Carriers / chemistry*
  • Drug Delivery Systems
  • Drug Liberation
  • Drug Stability
  • Drug Storage
  • Lipids / chemistry*
  • Nanoparticles*
  • Particle Size
  • Phosphatidylcholines / chemistry
  • Refrigeration
  • Stearic Acids / chemistry
  • alpha-Tocopherol / administration & dosage*
  • alpha-Tocopherol / chemistry

Substances

  • Delayed-Action Preparations
  • Drug Carriers
  • Lipids
  • Phosphatidylcholines
  • Stearic Acids
  • stearic acid
  • Chitosan
  • alpha-Tocopherol