Publication Date:
1989-05-12
Description:
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.〈br /〉〈span class="detail_caption"〉Notes: 〈/span〉Mukhopadhyay, A -- Chaudhuri, G -- Arora, S K -- Sehgal, S -- Basu, S K -- New York, N.Y. -- Science. 1989 May 12;244(4905):705-7.〈br /〉〈span class="detail_caption"〉Author address: 〈/span〉Institute of Microbial Technology, Chandigarh, India.〈br /〉〈span class="detail_caption"〉Record origin:〈/span〉 〈a href="http://www.ncbi.nlm.nih.gov/pubmed/2717947" target="_blank"〉PubMed〈/a〉
Keywords:
Albumins/*administration & dosage/metabolism
;
Animals
;
Cells, Cultured
;
Cricetinae
;
Female
;
Kinetics
;
Leishmania mexicana/*drug effects
;
Leishmaniasis/*drug therapy
;
Macrophages/metabolism/*parasitology
;
Male
;
*Membrane Proteins
;
Mesocricetus
;
Methotrexate/*administration & dosage/pharmacology/therapeutic use
;
*Receptors, Immunologic/metabolism
;
*Receptors, Lipoprotein
;
Receptors, Scavenger
;
Scavenger Receptors, Class B
;
Serum Albumin, Bovine
Print ISSN:
0036-8075
Electronic ISSN:
1095-9203
Topics:
Biology
,
Chemistry and Pharmacology
,
Computer Science
,
Medicine
,
Natural Sciences in General
,
Physics
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