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The molecular weight-dependence of tumour capture of N-(2-hydroxypropyl)methacrylamide (HPMA) copolymers (fractions of mw 22,000-778,000) was studied in vivo using subcutaneous (s.c.) Sarcoma 180 or B16F10 melanoma models. At 10 min, all fractions were already detectable in the tumour (1.5-3% of dose administered per gram) and those of molecular weight greater than the renal threshold showed progressive tumour accumulation up to 20% of dose administered per gram after 72 h in the Sarcoma 180 model. Tumour-selective uptake was confirmed for all copolymer fractions in both tumour models and in the sarcoma 180 model, the ratio (accumulation index, AI) of the AUC in tumour to AUC in skeletal muscle (a typical normal tissue) increasing from six to 12 with increasing copolymer molecular weight. The tumour/blood AI was greater (1-3) in the Sarcoma 180 model than the B16F10 melanoma model (0.4-1.0).

Original publication

DOI

10.1016/0959-8049(94)00514-6

Type

Journal article

Journal

Eur J Cancer

Publication Date

1995

Volume

31A

Pages

766 - 770

Keywords

Acrylamides, Animals, Drug Carriers, Iodine Radioisotopes, Macromolecular Substances, Male, Melanoma, Metabolic Clearance Rate, Mice, Molecular Weight, Neoplasms, Experimental, Sarcoma, Experimental, Tumor Cells, Cultured