Acta Pharm. 58 (2008) 287-297

full paper

Original research paper

 

A study of rivastigmine liposomes for delivery into brain through intranasal route

KARTHIK ARUMUGAM, GANESA SUNDARARAJAN SUBRAMANIAN, SURULIVEL RAJAN MALLAYASAMY, RANJITH KUMAR AVERINENI, MEKA SREENIVASA REDDY and NAYANABHIRAMA UDUPA

ganrajesh@gmail.com

Department of Pharmaceutical Quality Assurance, Manipal College of Pharmaceutical Sciences, Manipal, Karnataka-576 104, India

Accepted June 24, 2008

 

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 selectd as a model drug. Conventional liposomes were formulated by lipid layer hydration method using cholesterol and soya lecithin as lipid components. The concentration of rivastigmine in brain and plasma was studied in rat models after intranasal and oral administration of liposomes and free drug. 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.

 

Keywords: rivastigmine, liposomes, intranasal administration, brain drug delivery, pharmacokinetics