Program of Applied Chemistry, Graduate School of Advanced Science and Engineering, Hiroshima University, 1-4-1 Kagamiyama, Higashi, Hiroshima City 739-8527, Japan.
Program of Applied Chemistry, Graduate School of Advanced Science and Engineering, Hiroshima University, 1-4-1 Kagamiyama, Higashi, Hiroshima City 739-8527, Japan.
Nanomedicine. 2023 Apr;49:102659. doi: 10.1016/j.nano.2023.102659. Epub 2023 Feb 21.
Boron neutron capture therapy shows is a promising approach to cancer therapy, but the delivery of effective boron agents is challenging. To address the requirements for efficient boron delivery, we used a hybrid nanoparticle comprising a carborane = bearing pullulan nanogel and hydrophobized boron oxide nanoparticle (HBNGs) enabling the preparation of highly concentrated boron agents for efficient delivery. The HBNGs showed better anti-cancer effects on Colon26 cells than a clinically boron agent, L-BPA/fructose complex, by enhancing the accumulation and retention amount of the boron agent within cells in vitro. The accumulation of HBNGs in tumors, due to the enhanced permeation and retention effect, enabled the delivery of boron agents with high tumor selectivity, meeting clinical demands. Intravenous injection of boron neutron capture therapy (BNCT) using HBNGs decreased tumor volume without significant body weight loss, and no regrowth of tumor was observed three months after complete regression. The therapeutic efficacy of HBNGs was better than that of L-BPA/fructose complex. BNCT with HBNGs is a promising approach to cancer therapeutics.
硼中子俘获治疗是一种很有前途的癌症治疗方法，但有效硼试剂的递送具有挑战性。为了满足高效硼递药的要求，我们使用了一种包含载有碳化硼的普鲁兰纳米凝胶和疏水性氧化硼纳米颗粒的混合纳米颗粒（HBNGs），从而能够制备高浓度的硼试剂以实现高效递药。与临床硼试剂 L-BPA/果糖复合物相比，HBNGs 通过增强硼试剂在细胞内的积累和保留量，对 Colon26 细胞显示出更好的抗癌效果。由于增强的渗透和保留效应，HBNGs 在肿瘤中的积累能够实现高肿瘤选择性地递送硼试剂，满足临床需求。静脉注射硼中子俘获治疗（BNCT）用 HBNGs 降低了肿瘤体积，而体重没有明显减轻，在完全消退三个月后没有观察到肿瘤的再生长。HBNGs 的治疗效果优于 L-BPA/果糖复合物。HBNGs 的 BNCT 是癌症治疗的一种很有前途的方法。
