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Dr. Okun

Post of the Week: Methylesters of Levodopa for Treatment

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Dear forum members,


We have been watching levodopa methylester formulations especially as a treatment for delayed on's. This is a promising recent animal study:


Neurosci Lett. 2011 Aug 4. [Epub ahead of print]

Sustained-release formulation of levodopa methyl ester/benserazide for prolonged suppressing dyskinesia expression in 6-OHDA-leisoned rats.

Ren T, Yang X, Wu N, Cai Y, Liu Z, Yuan W.


School of Pharmacy, Shanghai Jiao Tong University, No. 800 Dongchuan Road, Shanghai 200240, China.


Although levodopa remains the most effective drug in the treatment of Parkinson's disease (PD), chronic administration of levodopa in the treatment of PD usually caused levodopa-induced dyskinesia (LID), the pathogenesis of which is poorly understood. It has been demonstrated that continuous dopamine stimulation reduces the expression of LID in PD. In the present study, levodopa methyl ester (LDME) and benserazide were microencapsulated into poly (lactide-co-glycolide) (PLGA) microspheres and then administrated to PD model of rats, which were induced by 6-hydroxydopamine injections. We found that both LDME/benserazide-loaded microspheres achieved sustained-release without burst release during the first day. LDME and benserazide had the same release slope from the second day on in vivo though benserazide released faster than LDME during the whole process. In our pharmacodynamic study, LDME/benserazide-loaded microspheres decreased apomorphine-induced turns and improved stepping of the lesioned forepaw in PD rats. Moreover, western blot analysis showed that the levels of ΔfosB, phosphorylated dopamine, cAMP-regulated phosphoprotein of 32kDa at threonine 34 and extracellular signal-regulated kinases 1 and 2 were decreased by LDME/benserazide-loaded microspheres in PD rats. These data showed that LDME/benserazide-loaded microspheres could be used to treat PD motor symptoms and ameliorate the expression of LID in this rat model of PD.


Copyright © 2011. Published by Elsevier Ireland Ltd.


PMID: 21835223 [PubMed - as supplied by publisher]

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