Zhang Yuanyuan, Li Qian, Hu Jinglu, Wang Chunqing, Wan Delian, Li Qi, Jiang Qingwei, Du Lina, Jin Yiguang
School of Pharmacy, Shandong University of Traditional Chinese Medicine, Jinan 250355, China.
Department of Pharmaceutical Sciences, Beijing Institute of Radiation Medicine, Beijing 100850, China.
Gels. 2022 Feb 10;8(2):108. doi: 10.3390/gels8020108.
(1) Background: When the body is exposed to microwave radiation, the brain is more susceptible to damage than other organs. However, few effective drugs are available for the treatment of microwave-induced brain injury (MIBI) because most drugs are difficult to cross the blood-brain barrier (BBB) to reach the brain. (2) Methods: Nasal cinnarizine inclusion complexes with thermo-and ion-sensitive hydrogels (cinnarizine ISGs) were prepared to treat MIBI and the characteristics of the inclusion complexes and their thermo-and ion-sensitive hydrogels were evaluated. (3) Results: Due to high viscosity, cinnarizine ISGs can achieve long-term retention in the nasal cavity to achieve a sustained release effect. Compared with the model, the intranasal thermo-and ion-sensitive cinnarizine ISGs significantly improved the microwave-induced spatial memory and spontaneous exploration behavior with Morris water maze and open field tests. Cinnarizine ISGs inhibited the expression of calcineurin and calpain 1 in the brain, which may be related to the inhibition of calcium overload by cinnarizine. (4) Conclusion: Intranasal thermo- and ion-sensitive cinnarizine ISGs are a promising brain-targeted pharmaceutical preparation against MIBI.
(1) 背景:当身体暴露于微波辐射时,大脑比其他器官更容易受到损伤。然而,由于大多数药物难以穿过血脑屏障(BBB)到达大脑,因此几乎没有有效的药物可用于治疗微波诱导的脑损伤(MIBI)。(2) 方法:制备了与热和离子敏感水凝胶的鼻用桂利嗪包合物(桂利嗪ISG)来治疗MIBI,并评估了包合物及其热和离子敏感水凝胶的特性。(3) 结果:由于高粘度,桂利嗪ISG可以在鼻腔中实现长期滞留以达到缓释效果。与模型组相比,鼻用热和离子敏感的桂利嗪ISG通过Morris水迷宫和旷场试验显著改善了微波诱导的空间记忆和自发探索行为。桂利嗪ISG抑制了大脑中钙调神经磷酸酶和钙蛋白酶1的表达,这可能与桂利嗪抑制钙超载有关。(4) 结论:鼻用热和离子敏感的桂利嗪ISG是一种有前景的针对MIBI的脑靶向药物制剂。