ABSTRACT

Targeted drug delivery is a promising strategy to improve both the efficacy and safety of treatment. This is especially attractive for cancer therapy as most anti-cancer drugs have only marginal therapeutic index. Folate receptor (FR) is selectively amplified on human malignant cells and can take up folate and its analogs through a receptor-mediated endocytosis process. FR-targeted liposomes can be utilized to deliver therapeutic agents to FR positive cells. The selective amplification of FR expression in both human solid tumors and leukemia suggests its utility as a potentially valuable target for drug and gene delivery. Preparation of folate receptor (FR) targeted liposomes is relatively straightforward since the targeting lipid component can simply be included into the lipid composition during the formation of liposomes. The area of FR targeting remains an area of great excitement, suggested by large number of recent publications and reports from industrial development.