Pharmacokinetic evaluation of formulated levodopa methyl ester nasal delivery systems

作者：Lee Yeon Hong; Kim Kyung Hee; Yoon In Kyung; Lee Kyung Eun; Chun In Koo; Rhie Jeong Yeon; Gwak Hye Sun^*

来源：European Journal of Drug Metabolism and Pharmacokinetics, 2014, 39(4): 237-242.

DOI：10.1007/s13318-013-0171-8

• Levodopa methyl ester
• Pharmacokinetics
• Nasal delivery

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.

• 出版日期2014-12