Huang Yichi, Li Jiaze, Wang Sen, Tian Hongqi, Fan Saijun, Zhao Yu
Tianjin Key Laboratory of Radiation Medicine and Molecular Nuclear Medicine, Institute of Radiation Medicine, Chinese Academy of Medical Sciences and Peking Union Medical College, Tianjin, 300192, China.
Kechow Pharma, Inc., Shanghai, 200131, China.
J Nanobiotechnology. 2025 Mar 22;23(1):236. doi: 10.1186/s12951-025-03276-3.
The widespread application of ionizing radiation (IR) in medicine, while beneficial, also poses potential risks that necessitate effective countermeasures. Both 2-(3-aminopropylamino) ethanethiol (WR-1065) and curcumin are recognized as radioprotective agents; however, their clinical utility is hindered by notable shortcomings that could be addressed through reactive oxygen species (ROS)-responsive amphiphilic nanomaterials. We introduced a newly synthesized poly (ethylene glycol) (PEG)-polycaprolactone (PCL) polymer integrated with diselenide bonds and curcumin (HOOC-SeSe-Cur-PEG-SeSe-Cur-PCL, PEG-Cur-SeSe-PCL). The resulting spherical nanoparticles (NPs), which self-assembled from this polymer, were uniform with an average diameter of 118 nm. As a carrier for WR-1065, these NPs demonstrated a loading capacity of 30.9% and an efficacy of 56.7%. Importantly, the degradation of WR-1065 within the NPs was minimal in gastric fluid, decreasing by only approximately 20% over a 6-hour period. The innovative aspect of these NPs is their design to destabilize in ROS-rich environments, facilitating the release of WR-1065 and curcumin. Indeed, the survival rate of mice increased to 50% when these NPs were orally administered prior to exposure to a lethal dose of whole-body irradiation (8 Gy). The radioprotective impact of WR-1065-loaded NPs was evident in the small intestine of irradiated mice, characterized by the amelioration of radiation-induced epithelial damage, reduction of DNA damage, and inhibition of the apoptotic pathway. Collectively, this oral nanocarrier system for WR-1065 and curcumin holds promise as a potential candidate for the prophylaxis and treatment of acute intestinal injuries induced by IR.
电离辐射(IR)在医学中的广泛应用虽然有益,但也带来了潜在风险,因此需要有效的应对措施。2-(3-氨丙基氨基)乙硫醇(WR-1065)和姜黄素都被认为是辐射防护剂;然而,它们的临床应用受到显著缺点的阻碍,而活性氧(ROS)响应性两亲纳米材料可以解决这些缺点。我们引入了一种新合成的聚乙二醇(PEG)-聚己内酯(PCL)聚合物,其整合了二硒键和姜黄素(HOOC-SeSe-Cur-PEG-SeSe-Cur-PCL,PEG-Cur-SeSe-PCL)。由这种聚合物自组装而成的球形纳米颗粒(NPs)均匀,平均直径为118纳米。作为WR-1065的载体,这些纳米颗粒的负载量为30.9%,效率为56.7%。重要的是,纳米颗粒内WR-1065在胃液中的降解最小,在6小时内仅下降约20%。这些纳米颗粒的创新之处在于它们设计成在富含ROS的环境中不稳定,从而促进WR-1065和姜黄素的释放。事实上,在暴露于致死剂量的全身照射(8 Gy)之前口服这些纳米颗粒时,小鼠的存活率提高到了50%。负载WR-1065的纳米颗粒的辐射防护作用在受辐照小鼠的小肠中很明显,其特征是辐射诱导的上皮损伤得到改善、DNA损伤减少以及凋亡途径受到抑制。总的来说,这种用于WR-1065和姜黄素的口服纳米载体系统有望成为预防和治疗由IR引起的急性肠道损伤的潜在候选物。