Pharmacokinetics and Anticancer Activity of Folic Acid-Functionalized Magnetic Nanoparticles

The theranostic potential of functionalized magnetic nanoparticles (MNPs) generates different possibilities for their medical application, including better control of toxicity and reduction of potential side effects. Aminosilane magnetic nanoparticles (MNP@NH₂) and their folic acid derivatives (MNP@FA) labeled by N-hydroxysuccinimide ester (IRDye 800CW) were evaluated for prospective use in the design of new diagnostic and treatment tools for colorectal cancer, using the DLD-1 cell culture system and an animal model of cancer xenograft. In cell culture, MNP@FA internalization and nuclear localization were associated with decreased cell viability and increased apoptosis rate. Independent of the application method, the presence of folic acid on the MNP surface resulted in more rapid elimination from mice, without non-specific accumulation in animal organs. Additionally, increased retention of MNP@FA, restriction of tumor growth, and Caspase-3 dependent apoptosis were observed in the mouse xenograft model of colorectal cancer. Rapid and preferential uptake of MNP@FA by cancer cells associated with their ability to eliminate and prevent cancer cell growth (reduction of tumor mass) indicates their potential for targeted cancer therapy with lower toxicity.