Li Jiacheng, Chen Ziteng, Wang Zhijie, Lv Linwen, Liu Qiuyang, Chang Yanan, Chen Kui, Xing Gengmei
Institute of High Energy Physics, Chinese Academy of Sciences, 19B YuquanLu, Shijingshan District, Beijing 100049, China.
CAS Key Lab for Biomedical Effects of Nanomaterials and Nanosafety, 19B YuquanLu, Shijingshan District, Beijing 100049, China.
Biomater Sci. 2025 Jun 10;13(12):3280-3297. doi: 10.1039/d5bm00068h.
The current clinical application of the boron drug boronophenylalanine (BPA) in BNCT faces various issues owing to its low boron loading (approximately 5%), which limits its therapeutic efficacy. Therefore, the development of boron drugs with higher boron contents is essential. Enhancing the boron content in boron drug materials is the focus of this study. Two-dimensional (2D) boron nitride-doped nano graphene (BNNG) with a high boron content of 24.97% ± 1.14% w/w was synthesized the chemical vapor deposition (CVD) method. The size of BNNG was controlled through gradient density centrifugation. Subsequently, a strategy was proposed that leveraged a boron-nitrogen co-doping process to enhance the boron content. The resulting BN nanosheets that were grown on graphene oxide (GO) exhibited an onion-like structure. To serve as a multifunctional delivery platform, B-enriched BNNG was dispersed in an aqueous solution through π-π interactions with pyrene methanol polyethylene glycol carboxylate (PPEG) to form BNNG@PPEG, thus becoming water-dispersible. The synthesized multifunctional BNNG@PPEG material satisfied the requirements for BNCT, chemotherapy, and PTT with a high photothermal conversion efficiency ( = 40.552%). Under 1 W cm laser irradiation, BNNG@PPEG generated a temperature of 55 °C, and the cell survival rate significantly decreased to 36.2% ± 3.5%. Meanwhile, the thermal property of BNNG-DOX@PPEG facilitated the controlled release of doxorubicin (DOX). Under neutron irradiation, the BNNG@PPEG complex exhibited significant antitumor activity, and the cell survival rate significantly decreased to 34.82% ± 6.1%.
硼药物硼代苯丙氨酸（BPA）目前在硼中子俘获疗法（BNCT）中的临床应用面临各种问题，因为其硼负载量较低（约5%），这限制了其治疗效果。因此，开发具有更高硼含量的硼药物至关重要。提高硼药物材料中的硼含量是本研究的重点。采用化学气相沉积（CVD）法合成了硼含量高达24.97%±1.14%（w/w）的二维（2D）氮化硼掺杂纳米石墨烯（BNNG）。通过梯度密度离心控制BNNG的尺寸。随后，提出了一种利用硼氮共掺杂过程来提高硼含量的策略。在氧化石墨烯（GO）上生长的所得BN纳米片呈现出洋葱状结构。为了作为多功能递送平台，富含硼的BNNG通过与芘甲醇聚乙二醇羧酸盐（PPEG）的π-π相互作用分散在水溶液中，形成BNNG@PPEG，从而变得可水分散。合成的多功能BNNG@PPEG材料满足了BNCT、化疗和光热疗法（PTT）的要求，具有高光热转换效率（ = 40.552%）。在1 W/cm激光照射下，BNNG@PPEG产生的温度为55°C，细胞存活率显著降至36.2%±3.5%。同时，BNNG-DOX@PPEG的热性能促进了阿霉素（DOX）的控释。在中子照射下，BNNG@PPEG复合物表现出显著的抗肿瘤活性，细胞存活率显著降至34.82%±6.1%。
