Nucleic acids delivery (gene therapy) has the unique potential to provide therapies for many incurable to date diseases [1-3]. The main problems in the gene therapy, however, are associated with poor transfection efficiency, cytotoxicity, immune response, drug loading and targeting delivery as well as ethical concerns and commercialization [1-3]. Therefore, in the last decades numerous of transporters for nucleic acids (vectors) were developed. Based on their design and properties, viral vectors currents show the best results in effective gene delivery. Alternatively, all other approaches are based on non-viral gene delivery systems, which try to mimic the efficiency of viral vectors by artificial means [4]. Our main strategy is based on building and self-generation of multifunctional nanostructures from commercially available or “easy to prepare” units, which will further self-assembled in complex, tuneable and multifunctional materials, suitable for specific targeted gene delivery and by this to overcome some existing issues [5-8]. On the other hand, nucleic acids and target cells are highly variable and therefore, rational design is limited to a relatively small number of components and a high number of synthetic steps, thus exploring dynamic chemistry and combinatorial approach for building nucleic acid vectors will provide a facile method to build large libraries of various compounds. In this communication, an overview related to preparation of libraries of non-viral vectors, characterization and self-assembly properties, nucleic acid binding properties, cytotoxicity and transfection efficiency is presented [5-8]. Vectors were build from lipid moiety, biocompatible polymers (PEG) and nucleic acid binding sites (PEI), liked all together to a core connector molecule through reversible dynamic imine bonds. It has been shown that obtained libraries of vectors have a good cell viability and a better transfection efficiency when compared to precursors [5-8].