Folate-conjugated liposomes preferentially target macrophages associated with ovarian carcinoma.
The folate receptor (FR) is overexpressed on many epithelial cancers and has been exploited for targeted delivery of folate-linked liposomes to cancer cells in vitro. The present studies investigate the distribution of folate-targeted liposomes in a FR(+) mouse model of ovarian cancer. According to flow cytometric analysis, folate-conjugation of liposomes significantly enhanced their uptake into ovarian cancer cells and tumor-associated macrophages within tumor ascites fluid. Compared to ovarian cancer cells, macrophages acquired tenfold more liposomes, and approximately 50% of this uptake was FR-dependent. These results demonstrate that, in addition to their cancer cell-targeting properties, folate-liposomes may be useful for targeting drugs to tumor-associated macrophages in vivo.
Turk
Mary Jo
MJ
Department of Chemistry, Purdue University, 560 Oval Drive, West Lafayette, IN 47907, USA.
Waters
David J
DJ
Low
Philip S
PS
D000818:Animals; D001201:Ascites; D002277:Carcinoma / Q000276:immunology* / Q000473:pathology* / Q000662:veterinary; D002352:Carrier Proteins / Q000494:pharmacology*; D004195:Disease Models, Animal; D016503:Drug Delivery Systems; D005260:Female; D005434:Flow Cytometry; D058973:Folate Receptors, GPI-Anchored; D005492:Folic Acid; D008081:Liposomes / Q000493:pharmacokinetics; D008264:Macrophages / Q000276:immunology*; D051379:Mice; D010051:Ovarian Neoplasms / Q000276:immunology* / Q000473:pathology* / Q000662:veterinary; D011956:Receptors, Cell Surface
D002352:Carrier Proteins; D058973:Folate Receptors, GPI-Anchored; D008081:Liposomes; D011956:Receptors, Cell Surface; D005492:Folic Acid