Integrin targeted drug and gene delivery.
BACKGROUND
Recently, there has been substantial progress in the development of integrin targeted pharmaceuticals and drug delivery systems. Integrin is an important member in the cell adhesion molecule family, which is involved in regulation of complex biological conditions, from keeping normal physiological activities to causing cellular dysfunction in diseased cells. Hence, it is timely to summarize the recent developments in integrin targeted drug and gene delivery systems to understand better their advantages and limitations.


METHODS
In this review, advances in the discovery and clinical trials of these integrin antagonists against different integrin subunits are summarized and discussed. Besides using integrin inhibitor as a single therapeutic agent, integrin antagonists that were conjugated to cytotoxic drugs by synthetic chemistry or coupled to biomacromolecules by either DNA recombination technology or fusion protein technology for integrin targeted therapy have been explored. Furthermore, nanoparticles with integrin targeting ligands for both drug and gene delivery, typically for antiangiogenesis and anticancer therapy, are highlighted and evaluated.


RESULTS
This review sheds light on the future development of integrin targeted drug and/or gene delivery systems.


CONCLUSIONS
Although thus far there are still limitations, integrin targeted delivery systems have already shown their potential as important pharmaceuticals in the near future.
Wang
Zhe
Z
National University of Singapore, Department of Pharmacy, 18 Science Drive 4, Singapore 117543, Singapore.
Chui
Wai-Keung
WK
Ho
Paul C
PC
D020533:Angiogenesis Inhibitors / Q000008:administration & dosage; D000818:Animals; D000906:Antibodies / Q000008:administration & dosage; D000970:Antineoplastic Agents / Q000008:administration & dosage; D016503:Drug Delivery Systems / Q000379:methods*; D004354:Drug Screening Assays, Antitumor; D018014:Gene Transfer Techniques; D006801:Humans; D016023:Integrins / Q000037:antagonists & inhibitors*; D015394:Molecular Structure; D053758:Nanoparticles / Q000008:administration & dosage* / Q000737:chemistry; D010455:Peptides / Q000008:administration & dosage; D016896:Treatment Outcome
D020533:Angiogenesis Inhibitors; D000906:Antibodies; D000970:Antineoplastic Agents; D016023:Integrins; D010455:Peptides