Abstract <p>Charged dendrimers are new polymeric structures that are distinguished by their high functionality, versatility in drug delivery, and well-defined structures—qualities that are comparable to those of biomolecules. These nanostructured macromolecules have shown their ability to entrap and/or conjugate high molecular weight hydrophilic/hydrophobic substances through host–guest interactions and covalent bonding (prodrug technique), respectively. Furthermore, they are a viable synthetic vector for gene transport due to their high surface group to molecular volume ratio. Because of these characteristics, charged dendrimers have captivated researchers in the creation of novel drug carriers and have been linked to several therapeutic and biological uses. Their toxicity concerns limit their employment in biological systems, despite their wide range of uses.</p> Lay Summary <p>In light of this, the current review has concentrated on the various approaches to their synthesis, drug delivery and targeting, gene delivery and other biomedical applications, interactions that contribute to the formation of drug-dendrimer complexes, characterization techniques used for their assessment, toxicity issues, and related strategies to mitigate their inherent toxicity.</p> Graphical Abstract <p></p>