Improved bioavailability of levodopa using floatable spray-coated microcapsules for the management of Parkinson’s disease
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 pe...
| Main Authors: | , , , , , , |
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| Format: | Journal Article |
| Language: | English |
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2019
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| Online Access: | https://hdl.handle.net/10356/92269 http://hdl.handle.net/10220/49468 |
| _version_ | 1826128945709318144 |
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| author | Baek, Jong-Suep Tee, Jie Kai Pang, Yi Yun Tan, Ern Yu Lim, Kah Leong Ho, Han Kiat Loo, Joachim Say Chye |
| author2 | School of Materials Science & Engineering |
| author_facet | School of Materials Science & Engineering Baek, Jong-Suep Tee, Jie Kai Pang, Yi Yun Tan, Ern Yu Lim, Kah Leong Ho, Han Kiat Loo, Joachim Say Chye |
| author_sort | Baek, Jong-Suep |
| collection | NTU |
| description | 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. |
| first_indexed | 2024-10-01T07:33:09Z |
| format | Journal Article |
| id | ntu-10356/92269 |
| institution | Nanyang Technological University |
| language | English |
| last_indexed | 2024-10-01T07:33:09Z |
| publishDate | 2019 |
| record_format | dspace |
| spelling | ntu-10356/922692023-07-14T15:53:43Z Improved bioavailability of levodopa using floatable spray-coated microcapsules for the management of Parkinson’s disease Baek, Jong-Suep Tee, Jie Kai Pang, Yi Yun Tan, Ern Yu Lim, Kah Leong Ho, Han Kiat Loo, Joachim Say Chye School of Materials Science & Engineering Singapore Centre for Environmental Life Sciences and Engineering Controlled Release DRNTU::Engineering::Materials Levodopa-induced Dyskinesia 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. MOE (Min. of Education, S’pore) Accepted version 2019-07-25T08:47:50Z 2019-12-06T18:20:21Z 2019-07-25T08:47:50Z 2019-12-06T18:20:21Z 2018 Journal Article 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 1535-1084 https://hdl.handle.net/10356/92269 http://hdl.handle.net/10220/49468 10.1007/s12017-018-8491-0 en NeuroMolecular Medicine © 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: http://dx.doi.org/10.1007/s12017-018-8491-0 23 p. application/pdf |
| spellingShingle | Controlled Release DRNTU::Engineering::Materials Levodopa-induced Dyskinesia Baek, Jong-Suep Tee, Jie Kai Pang, Yi Yun Tan, Ern Yu Lim, Kah Leong Ho, Han Kiat Loo, Joachim Say Chye Improved bioavailability of levodopa using floatable spray-coated microcapsules for the management of Parkinson’s disease |
| title | Improved bioavailability of levodopa using floatable spray-coated microcapsules for the management of Parkinson’s disease |
| title_full | Improved bioavailability of levodopa using floatable spray-coated microcapsules for the management of Parkinson’s disease |
| title_fullStr | Improved bioavailability of levodopa using floatable spray-coated microcapsules for the management of Parkinson’s disease |
| title_full_unstemmed | Improved bioavailability of levodopa using floatable spray-coated microcapsules for the management of Parkinson’s disease |
| title_short | Improved bioavailability of levodopa using floatable spray-coated microcapsules for the management of Parkinson’s disease |
| title_sort | improved bioavailability of levodopa using floatable spray coated microcapsules for the management of parkinson s disease |
| topic | Controlled Release DRNTU::Engineering::Materials Levodopa-induced Dyskinesia |
| url | https://hdl.handle.net/10356/92269 http://hdl.handle.net/10220/49468 |
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