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Science 12 May 1989:
Vol. 244. no. 4905, pp. 705 - 707
DOI: 10.1126/science.2717947

Articles

Science, Vol 244, Issue 4905, 705-707
Copyright © 1989 by American Association for the Advancement of Science


articles

Receptor-mediated drug delivery to macrophages in chemotherapy of leishmaniasis

A Mukhopadhyay, G Chaudhuri, SK Arora, S Sehgal, and SK Basu

Institute of Microbial Technology, Chandigarh, India.

Methotrexate coupled to maleylated bovine serum albumin was taken up efficiently through the "scavenger" receptors present on macrophages and led to selective killing of intracellular Leishmania mexicana amazonensis amastigotes in cultured hamster peritoneal macrophages. The drug conjugate was nearly 100 times as effective as free methotrexate in eliminating the intracellular parasites. Furthermore, in a model of experimental cutaneous leishmaniasis in hamsters, the drug conjugate brought about more than 90% reduction in the size of footpad lesions within 11 days. In contrast, the free drug at a similar concentration did not significantly affect lesion size. These studies demonstrate the potential of receptor-mediated drug delivery in the therapy of macrophage-associated diseases.


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V. Prasad, S. Hashim, A. Mukhopadhyay, S. K. Basu, and R. P. Roy (1999)
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