Evaluation of rat striatal L-dopa and DA concentration after intraperitoneal administration of L-dopa prodrugs in liposomal formulations

Journal of Controlled Release : Official Journal of the Controlled Release Society
Antonio Di StefanoEleonora Santucci

Abstract

Parkinson's disease is a neurodegenerative disease and its symptoms are relieved by administration of L-dopa (LD), which is converted by neuronal aromatic L-aminoacid decarboxylase (AADC), restoring dopamine (DA) levels in surviving neurons. In order to minimize unfavourable side effects, we studied new dimeric LD derivatives, as potential prodrugs for Parkinson's therapeutic treatment. To improve the bioavailability of the synthesized prodrugs, they were encapsulated in unilamellar liposomes of dimiristoylphosphatidylcholine (DMPC) and cholesterol (CHOL). In vivo microdialysis was used to monitor the striatal LD and DA concentrations after i.p. administration of new delivery systems. Bioavailability evaluation was performed by means of the HPLC-EC method. The striatal levels of LD and DA were remarkably elevated after i.p. administration of liposomal formulation of prodrug (+)-1b ([(O,O-diacetyl)-L-dopa-methylester]-succinyldiamide). This formulation showed about 2.5-fold increase in the basal levels of DA in dialysate rat striatum, suggesting that liposomal formulation of (+)-1b significantly increases LD and DA concentrations with respect to equimolar administration of LD itself or free prodrug (+)-1b.

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Citations

Dec 15, 2010·American Journal of Therapeutics·Congrong LinVasant Ranade
Aug 30, 2006·Proceedings of the National Academy of Sciences of the United States of America·Elizabeth J MeredithJohn Gordon
Nov 18, 2015·Journal of Liposome Research·Peter HinowIan G Tucker
Apr 23, 2009·Expert Opinion on Drug Delivery·Antonio Di StefanoLaura Serafina Cerasa
May 11, 2005·Expert Opinion on Investigational Drugs·Spiros Konitsiotis
Apr 13, 2012·Expert Opinion on Drug Discovery·Piera SozioAntonio Di Stefano
Nov 22, 2005·Expert Opinion on Drug Delivery·Tom H JohnstonJonathan M Brotchie
Jan 30, 2007·Progress in Neurobiology·Neha SinghYahya E Choonara
Feb 9, 2008·Molecules : a Journal of Synthetic Chemistry and Natural Product Chemistry·Antonio Di StefanoLaura Serafina Cerasa
Jan 4, 2018·Molecules : a Journal of Synthetic Chemistry and Natural Product Chemistry·Fatma HaddadRafik Karaman
Dec 5, 2009·Journal of Liposome Research·Maria CarafaEleonora Santucci
Dec 10, 2019·NPJ Parkinson's Disease·Vishakh IyerThyagarajan Subramanian
Nov 4, 2020·Journal of Neurology·Jonathan BaskinSimon J G Lewis
Aug 1, 2008·Journal of Medicinal Chemistry·Morteza MalakoutikhahErnest Giralt

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