ABSTRACT

Gene transfer is an emerging therapeutic modality for the treatment of cancer. Tumor-targeted gene delivery is a promising strategy for enhancing the efficacy of cancer gene therapy. The folate receptor (FR) is a 38 kDa membrane glycoprotein that is generally absent in normal tissues and is frequently amplified in human cancers. Folate-conjugated drug carriers, including gene transfer vectors, retain high affinity for the FR. As a low-molecular-weight ligand for tumor targeting, folate has many unique advantages, such as nonimmunogenicity and convenient availability, in addition to its high tumor specificity. A variety of gene transfer vectors have been conjugated to folate for folate-receptor-mediated tumor cell-specific delivery, including adenoviral particles, polyplexes, lipoplexes, and lipopolyplexes. In this review, recent reports on FR-targeted gene delivery are summarized. The potential applications of these vectors in cancer gene therapy are discussed.