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

Bastiat G, Plourde F, Motulsky A, Furtos A, Dumont Y, Quirion R, Fuhrmann G, Leroux JC (2010)

Publication Type: Journal article

Publication year: 2010


Book Volume: 31

Pages Range: 6031-6038

Journal Issue: 23

DOI: 10.1016/j.biomaterials.2010.04.009


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. © 2010 Elsevier Ltd.

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Bastiat, G., Plourde, F., Motulsky, A., Furtos, A., Dumont, Y., Quirion, R.,... Leroux, J.-C. (2010). Tyrosine-based rivastigmine-loaded organogels in the treatment of Alzheimer's disease. Biomaterials, 31(23), 6031-6038. https://dx.doi.org/10.1016/j.biomaterials.2010.04.009


Bastiat, Guillaume, et al. "Tyrosine-based rivastigmine-loaded organogels in the treatment of Alzheimer's disease." Biomaterials 31.23 (2010): 6031-6038.

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