A study of rivastigmine liposomes for delivery into the brain through intranasal route.
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.
Arumugam
Karthik
K
Department of Pharmaceutical Quality Assurance, Manipal College of Pharmaceutical Sciences, Manipal, Karnataka-576104 India.
Subramanian
Ganesa Sundararajan
GS
Mallayasamy
Surulivel Rajan
SR
Averineni
Ranjith Kumar
RK
Reddy
Meka Sreenivasa
MS
Udupa
Nayanabhirama
N
D000281:Administration, Intranasal; D000284:Administration, Oral; D000818:Animals; D001921:Brain / Q000378:metabolism*; D002626:Chemistry, Pharmaceutical; D002784:Cholesterol / Q000737:chemistry; D002800:Cholinesterase Inhibitors / Q000008:administration & dosage* / Q000097:blood / Q000737:chemistry / Q000493:pharmacokinetics; D002851:Chromatography, High Pressure Liquid; D004339:Drug Compounding; D054709:Lecithins / Q000737:chemistry; D008081:Liposomes; D008297:Male; D048448:Phenylcarbamates / Q000008:administration & dosage* / Q000097:blood / Q000737:chemistry / Q000493:pharmacokinetics; D051381:Rats; D017208:Rats, Wistar; D015203:Reproducibility of Results; D000068836:Rivastigmine; D013678:Technology, Pharmaceutical / Q000379:methods
D002800:Cholinesterase Inhibitors; D054709:Lecithins; D008081:Liposomes; D048448:Phenylcarbamates; D002784:Cholesterol; D000068836:Rivastigmine