2. Academic Validation
  3. Dual-Functional Nanoliposome with High BPA Loading for Targeted MRI-Guided BNCT of Glioblastoma

Dual-Functional Nanoliposome with High BPA Loading for Targeted MRI-Guided BNCT of Glioblastoma

  • ACS Appl Mater Interfaces. 2025 Sep 17;17(37):52474-52487. doi: 10.1021/acsami.5c11509.
Yaxin Qin 1,  Xiaoyan Sun 1,  Zhicheng Zhang 2,  Yufan Yang 1,  Qi Dai 2,  Xin Tan 1,  Ruolin Jiang 1,  Xiaoyan Bao 1,  Linjie Wu 1,  Changran Geng 3,  Yuanhao Liu 4,  Xiaoping Sun 4,  Xingyan Liu 4,  Minoru Suzuki 5,  Qinchun Wei 2,  Min Han 1 6
Affiliations

Affiliations

  • 1 Institute of Pharmaceutics, College of Pharmaceutical Sciences, Zhejiang University, Hangzhou 310058, PR China.
  • 2 Department of Radiation Oncology, Key Laboratory of Cancer Prevention and Intervention, The Second Affili-ated Hospital, Zhejiang University School of Medicine, Hangzhou 310058, China.
  • 3 Department of Nuclear Science and Technology, Nanjing University of Aeronautics and Astronautics, Nanjing 21106, China.
  • 4 Neuboron Therapy System Ltd., Xiamen 361020, PR China.
  • 5 Divison of Particle Radiation Oncology, Particle Radiation Oncology Research Center, Institute for Integrated Radiation and Nuclear Science, Kyoto University, Osaka 590-0494, Japan.
  • 6 Institute of Pharmaceutics, Zhejiang Province Key Laboratory of Anti-Cancer Drug Research, College of Pharmaceutical Sciences, Zhejiang University, Hangzhou 310058, PR China.
PMID: 40913548 DOI: 10.1021/acsami.5c11509
Abstract

Glioblastoma is a highly malignant brain tumor with few available therapeutic options, for which boron neutron capture therapy (BNCT) has emerged as a promising precision radiotherapy approach. However, its efficacy remains suboptimal due to inadequate tumor targeting of boron agents and lack of in vivo visualization. Herein, a gadolinium-boron integrated lipid nanocarrier (BPA-F&DOTA-Gd@LIPO-ANG) was developed for targeted boron delivery and MRI-guided BNCT. BPA-F and DOTA-Gd were coloaded into lipid nanocarriers using a microfluidic system, with Angiopep-2 modification to enhance blood-brain barrier penetration and glioma targeting. Following cellular uptake, BPA-F&DOTA-Gd@LIPO-ANG effectively increased boron accumulation in glioma cells, inducing significant Apoptosis and DNA damage upon neutron irradiation. Intravenously injected into orthotopic glioma model mice, BPA-F&DOTA-Gd@LIPO-ANG selectively accumulated in the tumor site, increasing tumor-to-normal tissue (T/N) and tumor-to-blood (T/B) ratios. Enhanced boron accumulation facilitated greater cytotoxic effects mediated by high-energy rays from the boron capture reaction, leading to significantly prolonged mice survival. In addition, in vitro and in vivo MRI validations confirmed its MRI visualization capability, meeting the demand for boron drug imaging for BNCT diagnosis and treatment integration. Overall, these results suggest that BPA-F&DOTA-Gd@LIPO-ANG is a promising targeted boron delivery system for MRI-guided BNCT in glioblastoma treatment.

Keywords

boron neutron capture therapy; dual-functional nanoliposome; glioma; magnetic resonance imaging; nano delivery system.

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