title: Galantamine-loaded solid-lipid nanoparticles for enhanced brain delivery: preparation, characterization, in vitro and in vivo evaluations.
abstract: Galantamine hydrobromide, a promising acetylcholinesterase inhibitor is reported to be associated with cholinergic side effects. Its poor brain penetration results in lower bioavailability to the target site. With an aim to overcome these limitations, solid-lipid nanoparticulate formulation of galantamine hydrobromide was developed employing biodegradable and biocompatible components. The selected galantamine hydrobromide-loaded solid-lipid nanoparticles offered nanocolloidal with size lower than 100 nm and maximum drug entrapment 83.42 ± 0.63%. In vitro drug release from these spherical drug-loaded nanoparticles was observed to be greater than 90% for a period of 24 h in controlled manner. In vivo evaluations demonstrated significant memory restoration capability in cognitive deficit rats in comparison with naive drug. The developed carriers offered approximately twice bioavailability to that of plain drug. Hence, the galantamine hydrobromide-loaded solid-lipid nanoparticles can be a promising vehicle for safe and effective delivery especially in disease like Alzheimer's.
authors.affiliation: a Department of Pharmacology , Post Graduate Institute of Medical Education and Research , Chandigarh , Punjab , India .
authors.forename: Shubham
authors.initials: S
authors.lastname: Misra
authors.affiliation: b Pharmacology Division, University Institute of Pharmaceutical Sciences, Panjab University , Chandigarh , Punjab , India , and.
authors.forename: Kanwaljit
authors.initials: K
authors.lastname: Chopra
authors.affiliation: c Pharmaceutics Division, University Institute of Pharmaceutical Sciences, Panjab University , Chandigarh , Punjab , India.
authors.forename: V R
authors.initials: VR
authors.lastname: Sinha
authors.affiliation: a Department of Pharmacology , Post Graduate Institute of Medical Education and Research , Chandigarh , Punjab , India .
authors.forename: Bikash
authors.initials: B
authors.lastname: Medhi
mesh_terms: D000818:Animals; D001921:Brain / Q000378:metabolism*; D002800:Cholinesterase Inhibitors / Q000737:chemistry* / Q000494:pharmacology*; D004337:Drug Carriers / Q000737:chemistry*; D016503:Drug Delivery Systems; D005702:Galantamine / Q000737:chemistry / Q000494:pharmacology*; D008055:Lipids / Q000737:chemistry*; D053758:Nanoparticles / Q000737:chemistry*; D051381:Rats
chemical_list: D002800:Cholinesterase Inhibitors; D004337:Drug Carriers; D008055:Lipids; D005702:Galantamine
keywords: Brain targeting; dementia; galantamine; memory; solid–lipid nanoparticles