Solid lipid nanoparticles carrying lipophilic derivatives of doxorubicin: preparation, characterization, and in vitro cytotoxicity studies

J Microencapsul. 2016 Jun;33(4):381-90. doi: 10.1080/02652048.2016.1202342. Epub 2016 Jun 29.

Abstract

Doxorubicin (DOXO) lauroyl ester and amide were proposed as lipophilic derivatives and entrapped in SLNs. DOXO derivatives-loaded SLNs were spherical shaped, had 200-300 nm mean diameters and showed 80-94% w/w drug entrapment efficiencies. The effect of DOXO derivatives-loaded SLNs and free DOXO on cell growth was examined by MTT and colony-forming assays on four different tumour cell lines: a pancreatic, CFPAC-1, a lung, A549, and two ovarian, A2780 and A2780res (DOXO-resistant). The results obtained with MTT and colony-forming assay show that although DOXO displayed an inhibition of cell proliferation greater or similar to DOXO lauroyl amide-loaded SLNs on all cell types, the effect induced by DOXO lauroyl ester-loaded SLNs was higher and concentration-dependent, and it was the only one maintained at 10(-5 )mM concentration. Only DOXO lauroyl ester-loaded SLNs were able to induce a 40% inhibitory effect on A2780 res cell line up to 10(-4 )mM concentration.

Keywords: Coacervation method; SLN; cytotoxicity; doxorubicin.

MeSH terms

  • Cell Line, Tumor
  • Cytotoxins* / chemistry
  • Cytotoxins* / pharmacokinetics
  • Cytotoxins* / pharmacology
  • Doxorubicin* / analogs & derivatives
  • Doxorubicin* / chemistry
  • Doxorubicin* / pharmacokinetics
  • Doxorubicin* / pharmacology
  • Drug Carriers* / chemistry
  • Drug Carriers* / pharmacokinetics
  • Drug Carriers* / pharmacology
  • Humans
  • Lipids* / chemistry
  • Lipids* / pharmacokinetics
  • Lipids* / pharmacology
  • Nanoparticles / chemistry*
  • Neoplasms / drug therapy*
  • Neoplasms / metabolism
  • Neoplasms / pathology

Substances

  • Cytotoxins
  • Drug Carriers
  • Lipids
  • Doxorubicin