A study of rivastigmine liposomes for delivery into the brain through intranasal route
A study of rivastigmine liposomes for delivery into the brain through intranasal route
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DOI：
10.2478/v10007-008-0014-3
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发表时间：
2008-09-01
影响因子：
2.8
通讯作者：
Udupa, Nayanabhirama
中科院分区：
文献类型：
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作者：
Arumugam, Karthik;Subramanian, Ganesa Sundararajan;Udupa, Nayanabhirama
目前的研究主要旨在通过鼻腔途径使用脂质体制剂将药物输送到大脑中。为此，用于治疗阿尔茨海默病的利瓦斯明被选为模型药物。以胆固醇和大豆卵磷脂为脂组分，采用脂层水合法制备了常规脂质体。采用大鼠鼻腔给药模型，研究了利凡斯的明鼻腔给药、游离给药和口服给药后大鼠脑内和血浆中的药物浓度。与鼻内游离药物和口服给药相比，鼻腔注射利凡斯明脂质体的脑内药物水平明显更高。鼻腔脂质体在脑内的半衰期比滴鼻或口服游离药物的半衰期更长。通过鼻腔给药来治疗阿尔茨海默病可能是治疗这种疾病的一种新方法。
The present study is mainly aimed at delivering a drug into the brain via the intranasal route using a liposomal formulation. For this purpose, rivastigmine, which is used in the management of Alzheimer's disease, was selected as a model drug. Conventional liposomes were formulated by the lipid layer hydration method using cholesterol and soya lecithin as lipid components. The concentration of rivastigmine in brain and plasma after intranasal liposomes, free drug and per oral administration was studied in rat models. A significantly higher level of drug was found in the brain with intranasal liposomes of rivastigmine compared to the intranasal free drug and the oral route. Intranasal liposomes had a longer half-life in the brain than intranasally or orally administered free drug. Delivering rivastigmine liposomes through the intranasal route for the treatment of Alzheimer's disease might be a new approach to the management of this condition.