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Review
. 2018 Nov;13(6):507-517.
doi: 10.1016/j.ajps.2017.11.004. Epub 2017 Dec 6.

Challenges and trends in apomorphine drug delivery systems for the treatment of Parkinson's disease

Nrupa Borkar  1 , Huiling Mu  1 , René Holm  2
Affiliations
Review

Challenges and trends in apomorphine drug delivery systems for the treatment of Parkinson's disease

Nrupa Borkar et al. Asian J Pharm Sci. 2018 Nov.

Abstract

Parkinson's disease (PD) is a chronic debilitating disease affecting approximately 1% of the population over the age of 60. The severity of PD is correlated to the degree of dopaminergic neuronal loss. Apomorphine has a similar chemical structure as the neurotransmitter dopamine and has been used for the treatment of advanced PD patients. In PD patients, apomorphine is normally administered subcutaneously with frequent injections because of the compound's extensive hepatic first-pass metabolism. There is, hence, a large unmet need for alternative administrative routes for apomorphine to improve patient compliance. The present review focuses on the research and development of alternative delivery of apomorphine, aiming to highlight the potential of non-invasive apomorphine therapy in PD, such as sublingual delivery and transdermal delivery.

Keywords: Alternative apomorphine therapy; Apomorphine; Drug delivery; Excipients; L-dopa, Levodopa; Non-invasive delivery; PAA-cys-2MNA, poly(acrylic acid)-cysteine-2-mercaptonicotinic acid; PD, Parkinson's disease; Parkinson's disease; SEDDS, Self-emulsifying drug delivery system.

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Figures

Image, graphical abstract
Graphical abstract
Fig. 1
Fig. 1
Chemical structures of R-(-)-apomorphine and dopamine.
Fig. 2
Fig. 2
General scheme of esterification of R-(-)-apomorphine to yield apomorphine diesters.
Fig. 3
Fig. 3
A graphical representation of APL-130277 bilayer sublingual strip formulation. Modified and reprinted with permission from Cynapsus Therapeutics, Inc. © Cynapsus Therapeutics, Inc., Toronto, Ontario, Canada.
Fig. 4
Fig. 4
A graphical representation of an iontophoretic patch. Modified from Green, 1996 .
See this image and copyright information in PMC

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