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Issue 13, 2018
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Y1 receptor ligand-based nanomicelle as a novel nanoprobe for glioma-targeted imaging and therapy

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Abstract

Due to the molecular and cellular heterogeneity of glioma, discovery of novel targeted sites and ligands for glioma imaging and therapy remains challenging. Neuropeptide Y (NPY) Y1 receptors (Y1Rs) are highly over expressed in various brain tumors including glioma, and can serve as potential targeting sites for glioma imaging and therapy. Here, we show by in vivo fluorescent imaging that a highly selective Y1R ligand, [Asn6, Pro34] NPY (AP-NPY), facilitated circumvention of the blood brain barrier (BBB) by nanomicelles specifically targeting glioma. Modification with AP-NPY stabilized doxorubicin-loaded nanomicelles in the normal physiological state and promoted drug release in the acidic tumor microenvironment. Furthermore, targeted delivery of AP-NPY nanomicelles improved the therapeutic efficacy of doxorubicin for glioma, producing a prolonged survival rate. These results suggest that Y1R is a novel targeted receptor, and its selective ligand AP-NPY improves BBB permeability and glioma targeting. Our study paves the way for developing a novel delivery system for diagnosis and treatment of glioma in which Y1Rs are over expressed.

Graphical abstract: Y1 receptor ligand-based nanomicelle as a novel nanoprobe for glioma-targeted imaging and therapy

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Publication details

The article was received on 07 Jan 2018, accepted on 26 Feb 2018 and first published on 06 Mar 2018


Article type: Communication
DOI: 10.1039/C8NR00148K
Citation: Nanoscale, 2018,10, 5845-5851
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    Y1 receptor ligand-based nanomicelle as a novel nanoprobe for glioma-targeted imaging and therapy

    J. Li, Y. Du, Z. Jiang, Y. Tian, N. Qiu, Y. Wang, M. Z. lqbal, M. Hu, R. Zou, L. Luo, S. Du, J. Tian and A. Wu, Nanoscale, 2018, 10, 5845
    DOI: 10.1039/C8NR00148K

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