Design and evaluation of levodopa methyl ester intranasal delivery systems

In Koo Chun, Yeon Hong Lee, Kyung Eun Lee, Hye Sun Gwak

Research output: Contribution to journalArticlepeer-review

11 Scopus citations


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.

Original languageEnglish
Pages (from-to)101-107
Number of pages7
JournalJournal of Parkinson's Disease
Issue number1
StatePublished - 2011


  • levodopa
  • Levodopa methyl ester
  • nasal delivery
  • permeation
  • stability


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