title: Preclinical studies of dendrimer prodrugs.
abstract: BACKGROUND
  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.
  
  
  METHODS
  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.
  
  
  CONCLUSIONS
  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.'
authors.affiliation: Osaka Prefecture University (OPU), Graduate School of Engineering, Department of Applied Chemistry , 1-1 Gakuen-cho, Naka-ku, Sakai, Osaka 599-8531 , Japan kojima@chem.osakafu-u.ac.jp.
authors.forename: Chie
authors.initials: C
authors.lastname: Kojima
mesh_terms: D000818:Animals; D000893:Anti-Inflammatory Agents / Q000008:administration & dosage / Q000737:chemistry / Q000493:pharmacokinetics; D000970:Antineoplastic Agents / Q000008:administration & dosage / Q000737:chemistry / Q000493:pharmacokinetics; D050091:Dendrimers / Q000737:chemistry*; D016503:Drug Delivery Systems; D015195:Drug Design; D004353:Drug Evaluation, Preclinical / Q000379:methods; D006801:Humans; D011092:Polyethylene Glycols / Q000737:chemistry; D011355:Prodrugs / Q000008:administration & dosage* / Q000737:chemistry / Q000493:pharmacokinetics; D012995:Solubility; D000068936:Theranostic Nanomedicine / Q000379:methods
chemical_list: D000893:Anti-Inflammatory Agents; D000970:Antineoplastic Agents; D050091:Dendrimers; D011355:Prodrugs; D011092:Polyethylene Glycols
keywords: anti-inflammatory; cancer therapy; dendrimer; ligand; prodrug; theranostics