A biodegradable nanocarrier system based on PLGA applicable for FR targeting is described. PEI‐based conjugates with covalently coupled folic acid are synthesized, characterized with regard to their composition and used for DNA complexation. The preparation of composites is performed by a solvent displacement technique, assuming an electrostatic interaction of PEI‐based polyplexes with PLGA. The synthesis of a folic acid‐PEG3kDa‐PEI25kDa conjugate is achieved. Blending of PLGA with polyplexes results in spherical nanoparticles with sizes ≤ 250 nm. Incorporation of polyplexes and the localization of folic acid on the particle surface, performed by antibody binding, is confirmed. The method is suitable for the preparation of nanosized, folic‐acid‐decorated nanoparticles.
