Doxorubicin-loaded phosphatidylethanolamine-conjugated nanoliposomes: in vitro characterization and their accumulation in liver, kidneys, and lungs in rats

Int J Nanomedicine. 2010 Oct 21;5:811-23. doi: 10.2147/IJN.S13031.


Introduction: Phosphatidylethanolamine (PE)-conjugated nanoliposomes were developed, characterized, and investigated for their accumulation in liver, kidneys, and lungs in rats.

Methods: Drug-excipient interaction was studied using Fourier transform infrared spectroscopy (FTIR), differential scanning calorimetry (DSC), surface morphology by field emission scanning electron microscopy, elemental analysis by energy dispersive X-ray (EDX) analysis, zeta potential and size distribution using a Zetasizer and particle size analyzer, and in vitro drug release by dialysis membrane. In vivo accumulation of liposomes in tissues was also studied.

Results: No chemical reaction was observed between drug and excipients. EDX study confirmed PE-conjugation in liposomes. Doxorubicin-loaded liposomes (DOX-L) and PE-conjugated doxorubicin-loaded liposomes (DOX-PEL) were of smooth surface and homogenously distributed in nanosize range (32-37 nm) with a negative surface charge. Loading efficiencies were 49.25% ± 1.05% and 52.98% ± 3.22% respectively, for DOX-L and DOX-PEL. In vitro drug release study showed 69.91% ± 1.05% and 77.07% ± 1.02% doxorubicin released, from DOX-L and DOX-PEL, respectively, in nine hours. Fluorescence microscopic study showed that liposomes were well distributed in liver, lungs, and kidneys.

Conclusion: Data suggests that PE-conjugated nanoliposomes released the drug in a sustained manner and were capable of distributing them in various organs. This may be used for cell/ tissue targeting, attaching specific antibodies to PE.

Keywords: doxorubicin; phosphatidylethanolamine-conjugated nanoliposomes; tissue accumulation.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Animals
  • Antibiotics, Antineoplastic / administration & dosage
  • Antibiotics, Antineoplastic / pharmacokinetics
  • Calorimetry, Differential Scanning
  • Doxorubicin / administration & dosage*
  • Doxorubicin / pharmacokinetics*
  • Drug Delivery Systems / methods*
  • Excipients
  • Fluorescein-5-isothiocyanate
  • Fluorescent Dyes
  • In Vitro Techniques
  • Kidney / metabolism
  • Liposomes / administration & dosage
  • Liposomes / chemistry
  • Liver / metabolism
  • Lung / metabolism
  • Microscopy, Electron, Scanning
  • Nanoconjugates / administration & dosage*
  • Nanoconjugates / chemistry*
  • Nanoconjugates / ultrastructure
  • Nanomedicine
  • Particle Size
  • Phosphatidylethanolamines / chemistry
  • Rats
  • Spectroscopy, Fourier Transform Infrared


  • Antibiotics, Antineoplastic
  • Excipients
  • Fluorescent Dyes
  • Liposomes
  • Nanoconjugates
  • Phosphatidylethanolamines
  • phosphatidylethanolamine
  • Doxorubicin
  • Fluorescein-5-isothiocyanate