Transdermal iontophoretic delivery of a novel series of dopamine agonists in vitro: physicochemical considerations

The Journal of Pharmacy and Pharmacology
O W AckaertJ A Bouwstra

Abstract

The transdermal iontophoretic delivery of a novel series of 2- aminotetralins and chromanamine-based dopamine agonists was investigated in vitro. Systematic structural modifications allowed us to investigate their effect on solubility in the donor phase and iontophoretic delivery across human skin. Transport profiles were analysed with nonlinear mixed effect modelling, utilizing an extension to an existing compartmental model. Furthermore, relationships between physicochemical properties and transport parameters were addressed. A solubility increase was observed: 5,6-di-OH-DPAT < 5-OH-MPAT < 5-OH-EPAT < 8-OH-DPAC. The structure significantly affected the iontophoretic delivery across human stratum corneum and dermatomed human skin with the highest flux for 5-OH-EPAT and 5-OH-MPAT. The extended model with two skin release constants (K(R1), K(R2)) described more adequately iontophoretic transport profiles than the existing model with one release constant. The extended model suggested two parallel transport pathways during current application. Across human stratum corneum, the electrophoretic mobility, measured with capillary electrophoresis, showed a linear relationship with the electromigrative flux and the zero-order iontophore...Continue Reading

References

Dec 1, 1979·Journal of Medicinal Chemistry·U HacksellD Sanchez
Nov 1, 1987·Naunyn-Schmiedeberg's Archives of Pharmacology·P M BeartA S Horn
Oct 1, 1984·European Journal of Pharmacology·M BeaulieuJ W Kebabian
Jan 10, 1998·Journal of Pharmaceutical Sciences·N G Turner, R H Guy
Feb 7, 1998·Pharmaceutical Research·R van der GeestH E Boddé
Oct 30, 1998·Pharmaceutical Research·M S RobertsY G Anissimov
Apr 1, 1999·Journal of Controlled Release : Official Journal of the Controlled Release Society·P M Lai, M S Roberts
Jan 12, 2002·Pharmaceutical Research·A Luzardo-AlvarezJ Blanco-Méndez
Oct 16, 2003·International Journal of Pharmaceutics·Gai Ling LiJoke A Bouwstra
Nov 7, 2003·Journal of Pharmaceutical Sciences·Asteria Luzardo-AlvarezJosé Blanco-Méndez
Jan 30, 2004·Annual Review of Medicine·C Warren Olanow
Apr 6, 2004·Journal of Controlled Release : Official Journal of the Controlled Release Society·Akhmad Kharis NugrohoJoke A Bouwstra
Jun 25, 2004·Journal of Chromatography. a·Salwa K PooleColin F Poole
Aug 7, 2004·European Journal of Pharmaceutics and Biopharmaceutics : Official Journal of Arbeitsgemeinschaft Für Pharmazeutische Verfahrenstechnik E.V·R Alvarez-RománR H Guy
Dec 14, 2004·Pharmaceutical Research·Akhmad Kharis NugrohoJoke A Bouwstra
Dec 14, 2004·Journal of Controlled Release : Official Journal of the Controlled Release Society·G L LiT van Laar
Mar 15, 2005·Journal of Controlled Release : Official Journal of the Controlled Release Society·Akhmad Kharis NugrohoJoke A Bouwstra
Apr 20, 2005·Pharmaceutical Research·Akhmad Kharis NugrohoJoke A Bouwstra
Sep 20, 2005·Pharmaceutical Research·Nada AblaYogeshvar N Kalia
Oct 19, 2005·Journal of Computer-aided Molecular Design·Igor V TetkoVolodymyr V Prokopenko
Nov 1, 2005·Journal of Pharmaceutical Sciences·Nada AblaYogeshvar N Kalia
May 30, 2006·Journal of Pharmaceutical Sciences·Akhmad Kharis NugrohoJoke A Bouwstra
Jul 14, 2006·European Journal of Pharmaceutical Sciences : Official Journal of the European Federation for Pharmaceutical Sciences·Yannic B SchuetzYogeshvar N Kalia
Sep 8, 2006·Movement Disorders : Official Journal of the Movement Disorder Society·John G Nutt
Aug 21, 2007·Journal of Controlled Release : Official Journal of the Controlled Release Society·Blaise MudryM Begoña Delgado-Charro
Apr 8, 2009·Journal of Controlled Release : Official Journal of the Controlled Release Society·Yveline HenchozPierre-Alain Carrupt
Sep 1, 2009·Journal of Pharmaceutical Sciences·Oliver W AckaertJoke A Bouwstra

❮ Previous
Next ❯

Citations

Oct 13, 2011·The Journal of Pharmacy and Pharmacology·Shinri TakasugaMine Kinoshita

❮ Previous
Next ❯

Related Concepts

Trending Feeds

COVID-19

Coronaviruses encompass a large family of viruses that cause the common cold as well as more serious diseases, such as the ongoing outbreak of coronavirus disease 2019 (COVID-19; formally known as 2019-nCoV). Coronaviruses can spread from animals to humans; symptoms include fever, cough, shortness of breath, and breathing difficulties; in more severe cases, infection can lead to death. This feed covers recent research on COVID-19.

Blastomycosis

Blastomycosis fungal infections spread through inhaling Blastomyces dermatitidis spores. Discover the latest research on blastomycosis fungal infections here.

Nuclear Pore Complex in ALS/FTD

Alterations in nucleocytoplasmic transport, controlled by the nuclear pore complex, may be involved in the pathomechanism underlying multiple neurodegenerative diseases including Amyotrophic Lateral Sclerosis and Frontotemporal Dementia. Here is the latest research on the nuclear pore complex in ALS and FTD.

Applications of Molecular Barcoding

The concept of molecular barcoding is that each original DNA or RNA molecule is attached to a unique sequence barcode. Sequence reads having different barcodes represent different original molecules, while sequence reads having the same barcode are results of PCR duplication from one original molecule. Discover the latest research on molecular barcoding here.

Chronic Fatigue Syndrome

Chronic fatigue syndrome is a disease characterized by unexplained disabling fatigue; the pathology of which is incompletely understood. Discover the latest research on chronic fatigue syndrome here.

Evolution of Pluripotency

Pluripotency refers to the ability of a cell to develop into three primary germ cell layers of the embryo. This feed focuses on the mechanisms that underlie the evolution of pluripotency. Here is the latest research.

Position Effect Variegation

Position Effect Variagation occurs when a gene is inactivated due to its positioning near heterochromatic regions within a chromosome. Discover the latest research on Position Effect Variagation here.

STING Receptor Agonists

Stimulator of IFN genes (STING) are a group of transmembrane proteins that are involved in the induction of type I interferon that is important in the innate immune response. The stimulation of STING has been an active area of research in the treatment of cancer and infectious diseases. Here is the latest research on STING receptor agonists.

Microbicide

Microbicides are products that can be applied to vaginal or rectal mucosal surfaces with the goal of preventing, or at least significantly reducing, the transmission of sexually transmitted infections. Here is the latest research on microbicides.