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盐酸美金刚纳米乳:治疗阿尔茨海默病的新方法。

Memantine nanoemulsion: a new approach to treat Alzheimer's disease.

机构信息

Department of Biotechnology, Jaypee Institute of Information Technology, Noida, India.

Nuclear Medicine Division, INMAS, Defence Research and Development Organization, New Delhi, India.

出版信息

J Microencapsul. 2020 Aug;37(5):355-365. doi: 10.1080/02652048.2020.1756971. Epub 2020 May 4.

Abstract

A nanoemulsion loaded with memantine for intranasal delivery to bypass the blood-brain barrier for the treatment of Alzheimer disease. The nanoemulsion was prepared using homogenisation and ultrasonication methods. The developed nanoemulsion was characterised, release and antioxidant potential was analysed. The studies were carried out by radiolabelling the memantine with technetium pertechnetate. The finalised NE showed particle-size of ∼11 nm and percentage transmittance of ∼99%. The release studies showed 80% drug release in simulated nasal fluid. The nanoemulsion showed 98% cell viability and antioxidative assays confirmed that the encapsulation of memantine in a nanoemulsion sustained its antioxidative potential. Gamma images and biodistribution results also confirmed higher uptake of formulation with %radioactivity of 3.6 ± 0.18%/g at 1.5 h in brains of rats administered intranasally. The developed nanoemulsion could be used as a potential carrier of memantine for a direct nose to brain delivery.

摘要

载有美金刚的纳米乳剂经鼻腔给药以绕过血脑屏障治疗阿尔茨海默病。纳米乳剂采用匀化和超声处理方法制备。对所开发的纳米乳剂进行了特性描述、释放和抗氧化潜力分析。通过放射性标记美金刚上的锝pertechnetate 进行研究。最终的 NE 显示出约 11nm 的粒径和约 99%的透射率。释放研究表明在模拟鼻液中释放了 80%的药物。纳米乳剂显示出 98%的细胞活力,抗氧化测定证实了将美金刚包封在纳米乳剂中可维持其抗氧化潜力。伽马图像和生物分布结果也证实,经鼻腔给予的大鼠脑内的制剂摄取率更高,给药后 1.5 小时的放射性标记%活性为 3.6±0.18%/g。所开发的纳米乳剂可用作美金刚的潜在载体,用于直接经鼻递送至大脑。

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