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Design and evaluation of levodopa methyl ester intranasal delivery systems

Title
Design and evaluation of levodopa methyl ester intranasal delivery systems
Authors
Chun I.K.Lee Y.H.Lee K.E.Gwak H.S.
Ewha Authors
곽혜선
SCOPUS Author ID
곽혜선scopus
Issue Date
2011
Journal Title
Journal of Parkinson's Disease
ISSN
1877-7171JCR Link
Citation
vol. 1, no. 1, pp. 101 - 107
Indexed
SCIE; SCOPUS WOS scopus
Abstract
Objectives: This study aimed to examine the feasibility of nasal powder formulations for the delivery of levodopa (L-dopa) into the brain using highly water-soluble levodopa methyl ester hydrochloride (LDME). Methods: For designing nasal LDME powders, pH-rate stabilities of LDME in buffer solutions and their enzymatic degradations in rabbit nasal mucosal and serosal extracts were investigated. In vitro permeation studies were carried out with four LDME nasal powders. Results: LDME was degraded fast in weakly acidic and neutral solutions, but relatively stable in acidic solutions. In nasal extracts, LDME (50 and 200 μg/mL) was rapidly hydrolyzed, forming L-dopa, and there were no significant differences in first-order degradation rates between mucosal and serosal extracts. From the in vitro permeation studies, LDME powder formulations resulted in faster appearance rates (1.07 ± 0.39 mg/cm2/hr) of L-dopa than solution formulations (0.35 ± 0.08 mg/cm2/hr). Conclusions: These results suggested that LDME nasal powder formulations could be useful delivery systems of L-dopa. © 2011 - IOS Press and the authors. All rights reserved.
DOI
10.3233/JPD-2011-10011
Appears in Collections:
약학대학 > 약학과 > Journal papers
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