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Cancer Lett. 2004 Sep 30;213(2):165-72.

Folate-conjugated liposomes preferentially target macrophages associated with ovarian carcinoma.

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Department of Chemistry, Purdue University, 560 Oval Drive, West Lafayette, IN 47907, USA.


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.

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