Folate-targeted liposomes for drug delivery

J. Lee Robert, Philip S. Low

Research output: Contribution to journalReview articlepeer-review

29 Scopus citations


The folate receptor has been identified as a marker for ovarian carcinomas and is also up-regulated in many other types of cancer. Folate- conjugation has been successfully applied in the tumor cell-selective targeting of liposomes. A long polyethyleneglycol (PEG) spacer between the targeting ligand (i.e. folio acid) and the liposome surface is required for receptor recognition. Ligand binding is compatible with the PEG-coating of the liposomes needed for prolonged systemic circulation. Folate-targeted liposomes have been shown to enhance the in vitro cytotoxicity of liposome- entrapped doxorubicin and antisense oligodeoxynucleotides to receptor- bearing tumor cells. Folate, as a targeting ligand, offers unique advantages over immunoliposomes, i.e., easy liposomal incorporation, low cost, high receptor affinity and tumor specificity, extended stability, and potential lack of immunogenicity.

Original languageEnglish (US)
Pages (from-to)455-466
Number of pages12
JournalJournal of Liposome Research
Issue number4
StatePublished - 1997

ASJC Scopus subject areas

  • Pharmaceutical Science


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