Physico-chemical characterisation, cytotoxic activity, and biocompatibility studies of tamoxifen-loaded solid lipid nanoparticles prepared via a temperature-modulated solidification method

J Microencapsul. 2014;31(6):590-9. doi: 10.3109/02652048.2014.898707. Epub 2014 Apr 3.

Abstract

Context: Solid lipid nanoparticles (SLNs) can efficiently and efficaciously incorporate anti-cancer agents.

Objective: To prepare and characterise tamoxifen (TAM)-loaded SLNs.

Materials and methods: Glyceryl monostearate, Tween-80, and trehalose were used in SLNs. SLNs were tested via dynamic light scattering (DLS), transmission electron microscopy (TEM), differential scanning calorimetry (DSC), X-ray diffraction (XRD), and Fourier transform infrared spectroscopy (FTIR).

Results: Characterisation studies revealed SLNs of about 540 nm with a negative surface charge and confirmed the entrapment of TAM in the SLNs. The entrapment efficiency was estimated to be 60%.

Discussion: The in vitro drug release profile demonstrated a gradual increase followed by a release plateau for several days. A drug concentration-dependent increase in cytotoxic activity was observed when the SLNs were evaluated in cell cultures.

Conclusion: Biocompatible and stable lyophilised SLNs were successfully prepared and found to possess properties that may be utilised in an anti-cancer drug delivery system.

Keywords: Biocompatibility; FTIR; X-ray powder diffractometry; dynamic light scattering; solid lipid nanoparticles; zeta potential.

MeSH terms

  • Antineoplastic Agents, Hormonal* / chemistry
  • Antineoplastic Agents, Hormonal* / pharmacokinetics
  • Antineoplastic Agents, Hormonal* / pharmacology
  • Delayed-Action Preparations / chemistry
  • Delayed-Action Preparations / pharmacokinetics
  • Delayed-Action Preparations / pharmacology
  • Glycerides* / chemistry
  • Glycerides* / pharmacokinetics
  • Glycerides* / pharmacology
  • Humans
  • Materials Testing*
  • Nanoparticles / chemistry*
  • Polysorbates* / chemistry
  • Polysorbates* / pharmacokinetics
  • Polysorbates* / pharmacology
  • Tamoxifen* / chemistry
  • Tamoxifen* / pharmacokinetics
  • Tamoxifen* / pharmacology
  • Trehalose* / chemistry
  • Trehalose* / pharmacokinetics
  • Trehalose* / pharmacology

Substances

  • Antineoplastic Agents, Hormonal
  • Delayed-Action Preparations
  • Glycerides
  • Polysorbates
  • Tamoxifen
  • glyceryl monostearate
  • Trehalose