Folic Acid-Conjugated Polymeric Nanoparticles for the DNA Active Targeting

Pharmaceutical carriers have been widely investigated in both laboratory and clinical settings to improve the efficiency of delivering therapeutic and diagnostic agents via different administration routes (1). Nano-drug delivery systems based on polymeric biomaterials have attracted considerable interest as drug delivery vehicles in recent decades (2). In this work new polyelectrolyte complex-based nanoparticles (NPs) were synthesized and characterized starting from methacrylic acid (MAA) and polyvinylpyrrolidone (PVP). The presence of PVP in the complex favors the interaction with nucleic acids and makes the nanoparticles able to elude the RES, thus increasing the circulation time (3). NPs were developed in the form of both nanospheres (NSs) and nanocapsules (NCs), an innovative kind of hollow nanoparticles with a great potential because of their low effective density and high specific surface area. Moreover, thanks to their internal cavity, NCs can maximize the amount of absorbed and released drug (4). Due to the fact that folic acid receptors exhibit limited expression on healthy cells but are often present in large number on cancer cells, NPs were functionalized using folic acid to obtained an active targeting towards cancer cells (5). Finally the ability of functionalized NPs to load and then release a nucleic acid was investigated