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Table 1.

Comparison of tumor pharmacokinetics of free doxorubicin versus liposomal formulations of doxorubicin

FormulationDoxil (16 mg/kg)
Doxil (9 mg/kg)
DOPC-PLD (9 mg/kg)
Free doxorubicin (9 mg/kg)
TotalNuclearTotalNuclearTotalNuclearTotalNuclear
AUC (μeq h/g tumor) 5,918 2,444 3,988 1,970 641 172 45.8 43.3 
% Bioavailable 41.3%  49.4%  26.8%  95.1%  
Cmax (μeq doxorubicin/g tumor) 48.8 25 28.6 15.9 11.9 11.4 7.9 2.9 
Tmax (h) 48 96 24 96 12 0.5 
t1/2 (h) 135 ND 151 ND 78 ND 25 ND 
MRT (h) 81 ND 81 ND 52 ND 10 ND 
Clearance (g/h/kg) 1.5 ND 1.1 ND 11.3 ND 89 ND 
FormulationDoxil (16 mg/kg)
Doxil (9 mg/kg)
DOPC-PLD (9 mg/kg)
Free doxorubicin (9 mg/kg)
TotalNuclearTotalNuclearTotalNuclearTotalNuclear
AUC (μeq h/g tumor) 5,918 2,444 3,988 1,970 641 172 45.8 43.3 
% Bioavailable 41.3%  49.4%  26.8%  95.1%  
Cmax (μeq doxorubicin/g tumor) 48.8 25 28.6 15.9 11.9 11.4 7.9 2.9 
Tmax (h) 48 96 24 96 12 0.5 
t1/2 (h) 135 ND 151 ND 78 ND 25 ND 
MRT (h) 81 ND 81 ND 52 ND 10 ND 
Clearance (g/h/kg) 1.5 ND 1.1 ND 11.3 ND 89 ND 

NOTE: Tumor levels of total doxorubicin and nuclear doxorubicin were determined in mice bearing orthotopic 4T1 mammary carcinomas following administration of 9 mg/kg doxorubicin as Doxil, DOPC-PLD, or free doxorubicin. Some mice also received 16 mg/kg of Doxil. AUC0-24 h for free doxorubicin and AUC0- 7d for liposomal doxorubicin formulations. All variables were determined using WinNonLin software.

Abbreviations: ND, no value determinable by the pharmacokinetic program; DOPC-PLD, dioleoylphosphatidylcholine/CHOL/mPEG2000-DSPE; MRT, mean residence time; μeq, microequivalents.

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