Aim: A nanoemulsion loaded with memantine for intranasal delivery to bypass the blood-brain barrier for the treatment of Alzheimer disease.

Method: The nanoemulsion was prepared using homogenisation and ultrasonication methods. The developed nanoemulsion was characterised, in vitro release and antioxidant potential was analysed. The in vivo studies were carried out by radiolabelling the memantine with technetium pertechnetate.

Results: The finalised NE showed particle-size of ∼11 nm and percentage transmittance of ∼99%. The in vitro 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.

Conclusion: The developed nanoemulsion could be used as a potential carrier of memantine for a direct nose to brain delivery.

目的：一种载有美金刚的纳米乳剂，用于鼻内输送，绕过血脑屏障，用于治疗阿尔茨海默氏病。

方法：采用均质和超声方法制备纳米乳液。表征了所开发的纳米乳液，在体外释放并分析了抗氧化剂的潜力。该体内研究是由放射性标记与锝高锝酸盐美金刚进行。

结果：最终的NE显示出〜11 nm的粒径和〜99％的透光率。该体外释放研究显示，在模拟鼻液80％的药物释放。纳米乳液显示出98％的细胞活力，抗氧化试验证实美金刚在纳米乳液中的包封可维持其抗氧化潜力。γ图像和生物分布结果还证实，鼻内给药的大鼠大脑在1.5 h时摄取的放射活性为3.6±0.18％/ g。

结论：开发的纳米乳剂可作为美金刚潜在的载体，用于直接将鼻子输送至大脑。