PMID: 8444658Jan 1, 1993Paper

Pharmacokinetics and biodistribution of methotrexate conjugated to mannosyl human serum albumin

The Journal of Antimicrobial Chemotherapy
R SettP K Das

Abstract

The superior efficacy of mannosylated neoglycoprotein-conjugated methotrexate, compared with free drug, in eliminating the parasite burden in both the in-vitro macrophage model and in-vivo mouse model of visceral leishmaniasis has been demonstrated previously. In the present study it was found that: (i) methotrexate conjugated to mannosyl human serum albumin (Man-HSA) was taken up rapidly by the liver and spleen, whereas the free drug was taken up by the kidney; (ii) uptake of the conjugate was ten-fold more efficient in liver macrophages (Kupffer cells) than in hepatocytes; (iii) most of the drug conjugate reached the lysosomes of Kupffer cells; and (iv) the active drug was released in the lysosomes of macrophages to act on Leishmania parasites.

Citations

Apr 28, 2006·Expert Opinion on Drug Delivery·Makiya Nishikawa, Mitsuru Hashida
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Mar 9, 2012·Biomaterials·Keerti JainNarendra K Jain
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