Interaction of methotrexate with polycationic carriers |
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Authors: | Stephen T. Chen Paul A. Kramer Dane O. Kildsig |
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Affiliation: | 1. Department of Industrial and Physical Pharmacy Purdue University West Lafayette, Indiana 47907, USA;2. Department of Pharmaceutics University of Connecticut Storrs, Connecticut 06268, USA |
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Abstract: | Binding parameters were measured for the interaction of methotrexate with poly-L-lysine and diethylaminoethyl dextran. The complexes were found to have apparent affinity constants of 2590 and 440 M?1 respectively at 37°, ionic strength 0.02. For hypotonic solutions containing therapeutic concentrations of methotrexate, this results in 87% binding of the drug to poly-L-lysine and 74% to diethylaminoethyl dextran. While the binding decreased to about 50% upon increasing ionic strength to physiologic levels, sufficient drug-carrying capacity was retained at isotonicity to support the potential utility of such complexes as tissue-specific drug carriers. |
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