Arumugam Karthik, Subramanian Ganesa Sundararajan, Mallayasamy Surulivel Rajan, Averineni Ranjith Kumar, Reddy Meka Sreenivasa, Udupa Nayanabhirama
Department of Pharmaceutical Quality Assurance, Manipal College of Pharmaceutical Sciences, Manipal, Karnataka-576104 India.
Acta Pharm. 2008 Sep;58(3):287-97. doi: 10.2478/v10007-008-0014-3.
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.
本研究主要旨在使用脂质体制剂通过鼻内途径将药物输送到大脑。为此，选择用于治疗阿尔茨海默病的卡巴拉汀作为模型药物。使用胆固醇和大豆卵磷脂作为脂质成分，通过脂质层水化法制备常规脂质体。在大鼠模型中研究了鼻内脂质体、游离药物和口服给药后大脑和血浆中卡巴拉汀的浓度。与鼻内游离药物和口服途径相比，发现鼻内给予卡巴拉汀脂质体后大脑中的药物水平显著更高。鼻内脂质体在大脑中的半衰期比鼻内或口服给予的游离药物更长。通过鼻内途径递送卡巴拉汀脂质体用于治疗阿尔茨海默病可能是管理这种疾病的一种新方法。
