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Tyrosine-based rivastigmine-loaded organogels in the treatment of Alzheimer’s disease

Paper ID Volume ID Publish Year Pages File Format Full-Text
9400 628 2010 8 PDF Available
Title
Tyrosine-based rivastigmine-loaded organogels in the treatment of Alzheimer’s disease
Abstract

Organogels can be prepared by immobilizing an organic phase into a three-dimensional network coming from the self-assembly of a low molecular weight gelator molecule. In this work, an injectable subcutaneous organogel system based on safflower oil and a modified-tyrosine organogelator was evaluated in vivo for the delivery of rivastigmine, an acetylcholinesterase (AChE) inhibitor used in the treatment of Alzheimer’s disease. Different implant formulations were injected and the plasmatic drug concentration was assayed for up to 35 days. In parallel, the inhibition of AChE in different brain sections and the biocompatibility of the implants were monitored. The pharmacokinetic profiles were found to be influenced by the gel composition, injected dose and volume of the implant. The sustained delivery of rivastigmine was accompanied by a significant prolonged inhibition of AChE in the hippocampus, a brain structure involved in memory. The implant induced only a minimal to mild chronic inflammation and fibrosis, which was comparable to poly(d,l-lactide-co-glycolide) in situ-forming implants. These findings suggest that tyrosine-based organogels could represent an alternative approach to current formulations for the sustained delivery of cholinesterase inhibitors.

Keywords
Organogel; Rivastigmine; Alzheimer’s disease; Pharmacokinetic; Biocompatibility; AChE inhibition
First Page Preview
Tyrosine-based rivastigmine-loaded organogels in the treatment of Alzheimer’s disease
Publisher
Database: Elsevier - ScienceDirect
Journal: Biomaterials - Volume 31, Issue 23, August 2010, Pages 6031–6038
Authors
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Subjects
Physical Sciences and Engineering Chemical Engineering Bioengineering