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Biotechnol Annu Rev. 2002;8:103-31.

Folate receptor-targeted liposomes as vectors for therapeutic agents.

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  • 1Division of Pharmaceutics and Pharmaceutical Chemistry, College of Pharmacy, Ohio State University, Columbus, OH 43210, USA.


The folate receptor is a cell surface protein that has recently been identified as a tumor marker, due to its differential overexpression in several malignancies. Current research indicates that folate can be covalently attached to the surface of liposomes to mediate their selective internalization by tumor cells through the folate receptor-mediated endocytic pathway. Optimized liposome formulations, characterized by improvements in drug loading, extended residence times in the circulation and improved drug release, have been developed to improve the biodistribution of therapeutic molecules. Theoretically, folate receptor-targeting can be combined with liposome encapsulation to synergistically affect disease outcome by enhancing the delivery of chemotherapeutic agents to neoplastic cells, while reducing systemic toxicities to normal tissues. The purpose of this chapter is to characterize the components of folate receptor-targeted liposomes, and summarize their applications in gene and drug delivery.

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