Cationization of drug products and carriers involves a direct modification
or attachment of conveying or accompanying components, either of which caus
e a charge modification. Cationization of macromolecules such as proteins a
nd nucleotides and particulate drug carriers generally enhances their cellu
lar uptake by endocytosis. The most common use of cationization today is in
gene delivery. This is undertaken by either employing cationic polymers or
entraping nucleotides in cationic carriers such as cationic liposomes. Cat
ionized delivery systems are also used to overcome biological barriers and
are suggested for drug targeting, in a nonspecific manner, to a variety of
body organs, including brain, eyes, nose, and inflamed intestinal epitheliu
m. Protein cationization is also suggested both for tumor immunotherapy and
as a diagnostic tool in cancer therapy. Cationization has proven itself to
be a straightforward tool for targeting to cells, tissues, and selected or
gans. This article reviews the extensive range of applications of cationiza
tion for improving drug and gene delivery and summarizes major technologies
employed for that purpose.