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Pharmacokinetic evaluation of formulated levodopa methyl ester nasal delivery systems. | LitMetric

Pharmacokinetic evaluation of formulated levodopa methyl ester nasal delivery systems.

Eur J Drug Metab Pharmacokinet

College of Pharmacy and Graduate School of Pharmaceutical Sciences, Ewha Womans University, 52 Ewhayeodae-gil, Seodaemun-Gu, Seoul, 120-750, Korea.

Published: December 2014

AI Article Synopsis

  • The study explored how well a nasal powder formulation of levodopa (LDME) delivers the drug to the brain compared to oral and intravenous methods.
  • Results showed that the nasal formulations had significantly higher bioavailability (82.4% with Carbopol and 66.7% without) versus only 16.2% for oral delivery.
  • The efficiency of targeting the drug to the brain was also much better with nasal formulations, indicating they are promising alternatives for delivering levodopa to treat conditions like Parkinson's disease.

Article Abstract

The objective of this study was to investigate the pharmacokinetic characteristics of levodopa (L-dopa) from nasal powder formulations using highly water-soluble levodopa methyl ester hydrochloride (LDME). In vivo pharmacokinetic studies were carried out with formulated LDME nasal powders. After oral and intravenous administration of L-dopa and carbidopa and intranasal administration LDME to the rat, L-dopa concentrations were determined in plasma and the brain using high-performance liquid chromatography. The absolute bioavailabilities of nasal preparations with and without Carbopol were 82.4 and 66.7 %, respectively, which were much higher than that of oral delivery (16.2 %). The drug-targeting efficiencies [area under the curve (AUC) in brain/AUC in plasma] of L-dopa in the nasal formulations (0.98-1.08) were much higher than that of oral preparation (0.69). These results suggest that LDME nasal powder formulations would be useful delivery systems of L-dopa to the brain.

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Source
http://dx.doi.org/10.1007/s13318-013-0171-8DOI Listing

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