The effect of dendrimers on the pharmacodynamic and pharmacokinetic behaviors of non-covalently or covalently attached drugs

Dendrimers are a new class of artificial macromolecules with several attractive properties that show promises in several biomedical applications. They can be widely used to increase the cellular uptake, bioavailability and therapeutic efficacy, to optimize the biodistribution and intracellular release profile, and to reduce the systemic toxicity, clearance and degradation rate of non-covalently or covalently attached drugs. Recent studies in this aspect clearly point to the potential advantages of dendrimers for the design of new drug delivery systems. Before final applications of dendrimer-based drug delivery systems in humans, we should not only address the benefits of these systems, but also assess the long-term pharmacodynamic (PD) and pharmacokinetic (PK) behaviors and health risk of them. In this mini-review, we will mainly discuss the influence of dendrimers on the PD and PK behaviors of drugs complexed or conjugated to them.

Potential pharmacokinetic profiles of (A) traditional dosing, (B) formulations of drug–dendrimer complexes, and (C) drug–dendrimer conjugates.Figure optionsDownload as PowerPoint slide