Folic acid-conjugated nanoparticles for targeted delivery to cancer cells

Abstract

Precise delivery of therapeutics to cancer cells is one of the greatest challenges in cancer therapy. Nanoparticles are potential carriers to deliver drugs into tumor cells with minimum drug leakage into normal cells. Conjugation of nanoparticles with ligands of cancer specific molecules such as folate, transferrin, hyaluronic acid, antibodies, peptides, aptamers and polysaccharides increase more specific drug targeting to cancer cells. Folic acid (FOL) is one of the most widely used targeting ligands for anticancer drugs due to its specificity and high binding affinity to the cancer cells. It provides additional advantages including ease of modification, good stability upon storage and low cost. Folic acid receptor is overexpressed on several cancer cell surfaces including ovarian, breast, lung, kidney, colorectal and brain cancers. Many studies demonstrate that FOL-decorated nanoparticles can improve efficacy and safety of anticancer drugs. In our recent studies, we found that the decoration of FOLconjugated polycaprolactone (PCL) and FOL-conjugated tocopheryl polyethylene glycol 1000 succinate (TPGS) onto methrotexate-conjugated PCL nanoparticles potentiated cytotoxicity and cellular uptake efficiency to folate receptor-expressed MCF-7 breast cancer cells.