Polymer-Coated Nanoparticles for Therapeutic and Diagnostic Non- 10 B Enriched Polymer-Coated Boron Carbon Oxynitride (BCNO) Nanoparticles as Potent BNCT Drug

• Published in: Nanomaterials (Basel, Switzerland) Switzerland), 2021-11, Vol.11 (11)
• Main Authors: Chiang, Chen-Wei, Chien, Yun-Chen, Yu, Wen-Jui, Ho, Chia-Yu, Wang, Chih-Yi, Wang, Tzu-Wei, Chiang, Chi-Shiun, Keng, Pei-Yuin
• Format: Article
• Language: English
• ISSN: 2079-4991; 2079-4991
• DOI: 10.3390/nano11112936

Boron neutron capture therapy (BNCT) is a powerful and selective anti-cancer therapy utilizing B-enriched boron drugs. However, clinical advancement of BCNT is hampered by the insufficient loading of B-10 drugs throughout the solid tumor. Furthermore, the preparation of boron drugs for BNCT relies on the use of the costly B-10 enriched precursor. To overcome these challenges, polymer-coated boron carbon oxynitride (BCNO) nanoparticles, with ~30% of boron, were developed with enhanced biocompatibility, cell uptake, and tumoricidal effect via BNCT. Using the ALTS1C1 cancer cell line, the IC of the PEG@BCNO, bare, PEI@BCNO were determined to be 0.3 mg/mL, 0.1 mg/mL, and 0.05 mg/mL, respectively. As a proof-of-concept, the engineered non- B enriched polymer-coated BCNO exhibited excellent anti-tumor effect via BNCT due to their high boron content per nanoparticle and due to the enhanced cellular internalization and retention compared to small molecular B-BPA drug. The astrocytoma ALTS1C1 cells treated with bare, polyethyleneimine-, and polyethylene glycol-coated BCNO exhibited an acute cell death of 24, 37, and 43%, respectively, upon 30 min of neutron irradiation compared to the negligible cell death in PBS-treated and non-irradiated cells. The radical approach proposed in this study addresses the expensive and complex issues of B-10 isotope enrichment process; thus, enabling the preparation of boron drugs at a significantly lower cost, which will facilitate the development of boron drugs for BNCT.