Table 7

Accumulation of liposomes in tumors

Animal and Tumor ModelFormulationDoseTimeAccumulation
mg/kg h μg/g
CD2F1 mice (P-1798 lymphosarcoma)7-a DaunoXome202439.57  ± 15.38
Free daunorubicin20242.02  ± 1.42
B6C3F1 mice (MA16C mammary adenocarcinoma)7-a DaunoXome202419.98  ± 8.77
Free daunorubicin20248.41  ± 1.11
Fischer rats (fibrous histiocytoma)7-b Doxil64810.92 
Free DOX640.8 
Female C3H/HeJ mice (FSa-R fibrosarcoma)7-c DSPC/Chol (55:45), 100 nm202416.3  ± 2.3
DSPC/Chol/PEG-DSPE (50:45:5)202415.7  ± 1.7
Free DOX2017.8  ± 3.1
Female C3H/HeJ mice (FSa-N fibrosarcoma)7-c DSPC/Chol (55:45), 100 nm202423.9  ± 2.7
DSPC/Chol/PEG-DSPE (50:45:5)202432.1  ± 4.7
Free DOX20112.8  ± 1.2
BDF1 mice (Lewis lung carcinoma)7-d DSPC/Chol (55:45), 100 nm55168143.8  ± 18.2
DSPC/Chol/PEG-DSPE (50:45:5)55168133.0  ± 11.9
Shionogi mice (SC115 mammary carcinoma)7-e TLC D-99132410.2  ± 3.6
6.5245.5  ± 1.1
6.5241.9  ± 0.08
BALB/c mice (M109 carcinoma)7-f Doxil5486.5  ± 4
104816  ± 17.3
204842  ± 39.3
Free DOX533.6  ± 2.1
1035.2  ± 2.1
BALB/c female mice (J6456 ascites)7-g PEG-DSPE/HSPC/Chol10245.9  ± 3.4
DSPG/HSPC/Chol10244.2  ± 2.95
HSPI/HSPC/Chol10245.3  ± 1.4
HSPC/Chol10241.8  ± 0.13
Free DOX1024<0.05
BALB/c female mice (M-109 carcinoma)7-g PEG-DSPE/HSPC/Chol102417.4  ± 8.8
DSPG/HSPC/Chol102417.4  ± 6.1
HSPC/Chol102419.7  ± 5.0
Free DOX10242.2  ± 0.6
mg/m2
Humans (various carcinomas)7-h Doxil253–7 days0.44
503–7 days0.69
Free DOX254–24 0.051
Humans (Kaposi's sarcoma lesions, biopsy specimens)7-i DaunoXome20241.07
40241.06
Humans (Kaposi's sarcoma lesions, biopsy specimens)7-j Doxil10722.06  ± 0.42
20721.61  ± 0.80
40727.71  ± 2.72
Free DOX10720.18  ± 0.07
20720.31  ± 0.16
40720.82  ± 0.18
  • The composition, size, and drug/lipid ratio for daunorubicin and DOX are listed in Table 1. When available, the time of analysis was the time of maximal accumulation.

  • 7-a Forssen et al. (1992).

  • 7-b Siegal et al. (1995).

  • 7-c Mayer et al. (1997).

  • 7-d Parr et al. (1997).

  • 7-e Mayer et al. (1990a).

  • 7-f Gabizon et al. (1997).

  • 7-g Gabizon et al. (1996).

  • 7-h Gabizon et al. (1994).

  • 7-i Forssen and Ross (1994).

  • 7-j Northfelt et al. (1996).