First Author | Sett R | Year | 1993 |
Journal | J Antimicrob Chemother | Volume | 31 |
Issue | 1 | Pages | 151-9 |
PubMed ID | 8444658 | Mgi Jnum | J:12244 |
Mgi Id | MGI:60494 | Doi | 10.1093/jac/31.1.151 |
Citation | Sett R, et al. (1993) Pharmacokinetics and biodistribution of methotrexate conjugated to mannosyl human serum albumin. J Antimicrob Chemother 31(1):151-9 |
abstractText | 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. |