Preclinical studies of dendrimer prodrugs

Abstract

Introduction: Dendrimers are synthetic macromolecules with well-defined structures bearing a wide variety of functional groups on their periphery. These groups can be used to conjugate bioactive molecules such as drugs, ligands and imaging agents. Dendrimer prodrugs can be used to improve the water solubility and pharmacokinetic properties of the corresponding free drugs.

Areas covered: This article summarizes preclinical studies pertaining to the use of drug–dendrimer conjugates as dendrimer prodrugs for the treatments of various diseases, including cancer and inflammatory diseases. A wide range of anticancer drugs have been conjugated to dendrimers via biodegradable linkers. The side effects of the parent drugs can be markedly reduced using dendrimer prodrugs, with some drugs showing improved efficacy. Anti-inflammatory agents have also been conjugated to dendrimers and used to treat a number of inflammatory diseases.

Expert opinion: Drug–dendrimer conjugates are preferable to drug–dendrimer complexes, where the use of degradable linkers is critical to the release of the drug. Polyethylene glycol and/or ligands can be added to a dendrimer prodrug, which is useful for the targeting of affected tissues. Imaging probes can also be incorporated into dendrimer prodrugs for the simultaneous delivery of therapeutic and diagnostic agents as ‘theranostics.’

Keywords:

• anti-inflammatory
• cancer therapy
• dendrimer
• ligand
• prodrug
• theranostics

Acknowledgments

I thank Ms Mariko Mitsui for her help in figure preparation and reference arrangement.

Declaration of interest

The author was supported by a grant-in-aid from the Japan Society for the Promotion of Science (JSPS) (No. 26410227). The author has no other relevant affiliations or financial involvement with any organization or entity with a financial interest in or financial conflict with the subject matter or materials discussed in the manuscript apart from those disclosed.

Notes

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