Formulation and in vitro/in vivo evaluation of levodopa transdermal delivery systems

Kyung Eun Lee, Yun Jung Choi, Byu Ree Oh, In Koo Chun, Hye Sun Gwak

Research output: Contribution to journalArticlepeer-review

14 Scopus citations

Abstract

This study aims to investigate the feasibility of Levodopa transdermal delivery systems (TDSs). Levodopa TDSs were formulated using various vehicles and permeation enhancers, and in vitro permeation and in vivo pharmacokinetic studies were carried out. In the in vitro study, ester-type vehicles showed relatively high enhancing effects; propylene glycol monocaprylate and propylene glycol monolaurate showed the highest permeation fluxes from both solution and pressure sensitive adhesive (PSA) TDS formulations. Lag time was dramatically shortened with PSA TDS formulations as compared with solution formulations. In the in vivo study, the addition of fatty acids increased blood drug concentrations regardless of the kind or concentration of fatty acid; the AUCinf increased up to 8.7 times as compared with propylene glycol (PG) alone. PSA TDS containing 10% linoleic acid exhibited prolonged T max as compared with oral form. Total clearance of L-dopa from PSA TDSs was significantly lower than from oral form (up to 86.8 times). Especially, PSA TDS containing 10% linoleic acid (LOA) revealed 76.2 fold higher AUC inf than oral administration. Based on our results, the L-dopa PSA TDS containing PG with 10% LOA could be used as a good adjuvant therapy for Parkinson's disease patients who experience symptom fluctuation by L-dopa oral administration.

Original languageEnglish
Pages (from-to)432-436
Number of pages5
JournalInternational Journal of Pharmaceutics
Volume456
Issue number2
DOIs
StatePublished - 2013

Keywords

  • Levodopa
  • Permeation
  • Pharmacokinetics
  • Transdermal delivery system

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