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

Juan Li; Yang Du; Zhenqi Jiang; Yuchen Tian; Nianxiang Qiu; Yinjie Wang; Muhammad Zubair lqbal; Menying Hu; Ruifen Zou; Lijia Luo; Shiyu Du; Jie Tian; Aiguo Wu

doi:10.1039/C8NR00148K

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

Juan Li,‡^a Yang Du,‡^b Zhenqi Jiang,^ac Yuchen Tian,^a Nianxiang Qiu,^a Yinjie Wang,^ac Muhammad Zubair lqbal,^a Menying Hu,^a Ruifen Zou,^ac Lijia Luo,^ac Shiyu Du,

^a Jie Tian*^b and Aiguo Wu

*^a

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* Corresponding authors

^a CAS Key Laboratory of Magnetic Materials and Devices, Key Laboratory of Additive Manufacturing Materials of Zhejiang Province, and Division of Functional Materials and Nanodevices, Ningbo Institute of Materials Technology and Engineering, Chinese Academy of Sciences, Ningbo 315201, China
E-mail: aiguo@nimte.ac.cn

^b CAS Key Laboratory of Molecular Imaging, The Sate Key Laboratory of Management and Control for Complex Systems, Institution of Automation, Chinese Academy of Sciences, Beijing 100190, China
E-mail: jie.tian@ia.ac.cn

^c University of Chinese Academy of Sciences, Beijing 100049, China

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.

Nanoscale

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

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

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