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Title: Improved bioavailability of levodopa using floatable spray-coated microcapsules for the management of Parkinson’s disease
Authors: Baek, Jong-Suep
Tee, Jie Kai
Pang, Yi Yun
Tan, Ern Yu
Lim, Kah Leong
Ho, Han Kiat
Loo, Joachim Say Chye
Keywords: Controlled Release
Levodopa-induced Dyskinesia
Issue Date: 2018
Source: Baek, J.-S., Tee, J. K., Pang, Y. Y., Tan, E. Y., Lim, K. L., Ho, H. K., & Loo, J. S. C. (2018). Improved bioavailability of levodopa using floatable spray-coated microcapsules for the management of Parkinson’s disease. NeuroMolecular Medicine, 20(2), 262-270. doi:10.1007/s12017-018-8491-0
Series/Report no.: NeuroMolecular Medicine
Abstract: Oral administration of levodopa (LD) is the gold standard in managing Parkinson’s disease (PD). Although LD is the most effective drug in treating PD, chronic administration of LD induces levodopa-induced dyskinesia. A continuous and sustained provision of LD to the brain could, therefore, reduce peak-dose dyskinesia. In commercial oral formulations, LD is co-administrated with an AADC inhibitor (carbidopa) and a COMT inhibitor (entacapone) to enhance its bioavailability. Nevertheless, patients are known to take up to five tablets a day because of poor sustained-releasing capabilities that lead to fluctuations in plasma concentrations. To achieve a prolonged release of LD with the aim of improving its bioavailability, floatable spray-coated microcapsules containing all three PD drugs were developed. This gastro-retentive delivery system showed sustained release of all PD drugs, at similar release kinetics. Pharmacokinetics study was conducted and this newly developed formulation showed a more plateaued delivery of LD that is void of the plasma concentration fluctuations observed for the control (commercial formulation). At the same time, measurements of LD and dopamine of mice administered with this formulation showed enhanced bioavailability of LD. This study highlights a floatable, sustained-releasing delivery system in achieving improved pharmacokinetics data compared to a commercial formulation.
ISSN: 1535-1084
DOI: 10.1007/s12017-018-8491-0
Schools: School of Materials Science & Engineering 
Research Centres: Singapore Centre for Environmental Life Sciences and Engineering 
Rights: © 2018 Springer Science+Business Media US. All rights reserved.This is a post-peer-review, pre-copyedit version of an article published in NeuroMolecular Medicine. The final authenticated version is available online at:
Fulltext Permission: open
Fulltext Availability: With Fulltext
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