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Int J Nanomedicine. 2012;7:4533-44. doi: 10.2147/IJN.S34450. Epub 2012 Aug 15.

Intracellular CXCR4⁺ cell targeting with T22-empowered protein-only nanoparticles.

Author information

1
Institut de Biotecnologia i de Biomedicina, Universitat Autònoma de Barcelona, Bellaterra, Barcelona, Spain.

Abstract

BACKGROUND:

Cell-targeting peptides or proteins are appealing tools in nanomedicine and innovative medicines because they increase the local drug concentration and reduce potential side effects. CXC chemokine receptor 4 (CXCR4) is a cell surface marker associated with several severe human pathologies, including colorectal cancer, for which intracellular targeting agents are currently missing.

RESULTS:

Four different peptides that bind CXCR4 were tested for their ability to internalize a green fluorescent protein-based reporter nanoparticle into CXCR4⁺ cells. Among them, only the 18 mer peptide T22, an engineered segment derivative of polyphemusin II from the horseshoe crab, efficiently penetrated target cells via a rapid, receptor-specific endosomal route. This resulted in accumulation of the reporter nanoparticle in a fully fluorescent and stable form in the perinuclear region of the target cells, without toxicity either in cell culture or in an in vivo model of metastatic colorectal cancer.

CONCLUSION:

Given the urgent demand for targeting agents in the research, diagnosis, and treatment of CXCR4-linked diseases, including colorectal cancer and human immunodeficiency virus infection, T22 appears to be a promising tag for the intracellular delivery of protein drugs, nanoparticles, and imaging agents.

KEYWORDS:

CXCR4; colorectal cancer; intracellular targeting; nanoparticles; peptide tag; self-assembling

PMID:
22923991
PMCID:
PMC3423154
DOI:
10.2147/IJN.S34450
[Indexed for MEDLINE]
Free PMC Article

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