Conventional therapies of several diseases, in particular cancer therapy, have been insufficient clinically for effective and safe treatment of these important diseases. The major cause of side effects is insufficient uptake and non-selective delivery of therapeutic molecules. In order to overcome this problem, colloidal, nano-sized carrier systems have been developed for gene and drug delivery. These novel delivery systems have a wide range of modification capabilities, such as controllable particle size and surface charge or grafting of different molecules for active or passive targeting to cells. A variety of modification or formulation approaches ensure the efficacy, equality and safety of the system. In this context, cationic nano-sized drug delivery systems have a net positive surface charge, suggesting strong cellular interactions with negatively charged biological membranes. This electrostatic interaction between cationic nanoparticles and cell membranes brings with it enhanced uptake of nanoparticles by cells. Another important advantage of cationic nanocarriers is that they are able to condense DNA, siRNA, nucleotides, peptides and proteins to form polyplexes that are able to deliver their load intracellularly, resulting in increased transfection efficiency. In this chapter the surface properties, cellular interaction and uptake mechanism of nano-sized drug carrier systems and the innovations in treatment are described using examples from the literature. In addition, various cationic polymers commonly used in drug and gene delivery and their characteristics are summarized. Positively charged nanocarrier systems emerge as a promising option for effective drug or gene therapy and extensive research is being carried out in this field worldwide.