Using a nanotech drug delivery method to target cancer cells is much more effective than using the drug by itself. In laboratory tests, nanoparticles that include a small molecule of nucleic acid that binds to a target molecule on prostate cancer cells were used to carry a lethal dose of the drug into the cancer cells without affecting cells lacking the cancer-specific target. From the National Cancer Institute’s Alliance for Nanotechnology in Cancer “Targeted Nanoparticles Boost Platinum-Based Anticancer Therapy“:

A research team from the Massachusetts Institute of Technology (MIT)-Harvard Center for Nanotechnology Excellence has custom-designed nanoparticles that can deliver the anticancer drug cisplatin specifically to prostate cancer cells. The nanoparticles are composed of two different polymers and are decorated with a nucleic acid aptamer that binds to the tumor marker prostate-specific membrane antigen. This aptamer ensures that the nanoparticles deliver their payload only to prostate cancer cells.

Stephen Lippard, Ph.D., and Robert Langer, Ph.D., MIT, and Omid Farokhzad, M.D., Harvard Medical School, led the team that developed this new formation of cisplatin. The investigators published their results in the Proceedings of the National Academy of Sciences of the United States of America [abstract].

To construct a stable nanoparticle that would only release its toxic cargo inside tumor cells, the investigators synthesized a modified version of cisplatin that includes a long hydrocarbon chain. As the nanoparticle forms, the hydrocarbon chain associates strongly with the hydrophobic chains of the polymer that forms the nanoparticle’s core. The researchers note that the hydrocarbon chain they chose optimizes both drug encapsulation and drug release inside tumor cells. Once the nanoparticle enters the cell, the modified drug is converted into its active form as a result of chemical conditions inside the cell.

Tests with human cancer cells growing in culture showed that these nanoparticles were taken up specifically by tumor cells and not by healthy cells. Nanoparticles lacking the targeting aptamer were not taken up either. These tests also demonstrated that the nanoparticles release their cargo over the course of 60 hours, providing a sustained lethal level of the drug inside the targeted cells. In addition, the nanoparticle formulation was approximately 100 times more effective at killing tumor cells than was cisplatin by itself.

—Jim