Efficacy of oral lipid-based formulations of apomorphine and its diester in a Parkinson's disease rat model

Research output: Contribution to journalJournal articleResearchpeer-review

Standard

Efficacy of oral lipid-based formulations of apomorphine and its diester in a Parkinson's disease rat model. / Borkar, Nrupa; Andersson, Daniel R.; Yang, Mingshi; Müllertz, Anette; Holm, René; Mu, Huiling.

In: Journal of Pharmacy and Pharmacology, Vol. 69, No. 9, 09.2017, p. 1110-1115.

Research output: Contribution to journalJournal articleResearchpeer-review

Harvard

Borkar, N, Andersson, DR, Yang, M, Müllertz, A, Holm, R & Mu, H 2017, 'Efficacy of oral lipid-based formulations of apomorphine and its diester in a Parkinson's disease rat model', Journal of Pharmacy and Pharmacology, vol. 69, no. 9, pp. 1110-1115. https://doi.org/10.1111/jphp.12758

APA

Borkar, N., Andersson, D. R., Yang, M., Müllertz, A., Holm, R., & Mu, H. (2017). Efficacy of oral lipid-based formulations of apomorphine and its diester in a Parkinson's disease rat model. Journal of Pharmacy and Pharmacology, 69(9), 1110-1115. https://doi.org/10.1111/jphp.12758

Vancouver

Borkar N, Andersson DR, Yang M, Müllertz A, Holm R, Mu H. Efficacy of oral lipid-based formulations of apomorphine and its diester in a Parkinson's disease rat model. Journal of Pharmacy and Pharmacology. 2017 Sep;69(9):1110-1115. https://doi.org/10.1111/jphp.12758

Author

Borkar, Nrupa ; Andersson, Daniel R. ; Yang, Mingshi ; Müllertz, Anette ; Holm, René ; Mu, Huiling. / Efficacy of oral lipid-based formulations of apomorphine and its diester in a Parkinson's disease rat model. In: Journal of Pharmacy and Pharmacology. 2017 ; Vol. 69, No. 9. pp. 1110-1115.

Bibtex

@article{9f60dbd531e64880a422fca3eeb49e83,
title = "Efficacy of oral lipid-based formulations of apomorphine and its diester in a Parkinson's disease rat model",
abstract = "ObjectivesApomorphine is used to symptomatically treat Parkinson's disease (PD). Oral delivery of apomorphine is generally limited by its short plasma half-life and a hepatic first-pass metabolism. This study was aimed at evaluating the behavioural response of apomorphine and its prodrug administered in oral lipid-based formulations.MethodsThe behavioural response of apomorphine and its prodrug administered in oral lipid-based formulations was evaluated using a 6-hydroxydopamine-lesioned rat model simulating PD symptomatology. Apomorphine or dipalmitoyl apomorphine (DPA) was incorporated into different lipid-based formulations and orally administered (0.24 mmol/kg) to the PD rat model. The rotations by the rats were counted.Key findingsThe duration of response lasted to about 2.5 h with oral apomorphine- and DPA-loaded o/w emulsion, while it was increased to 6 h when DPA was incorporated in self-emulsifying drug delivery systems compared to s.c. apomorphine (1 h). This suggests that the lipid-based formulations provide a sustained drug release allowing for a steady exposure to the brain.ConclusionsOral lipid-based apomorphine delivery has a potential in achieving a steady response, though at a higher dose possibly eliminating the need for frequent s.c. apomorphine administration.",
author = "Nrupa Borkar and Andersson, {Daniel R.} and Mingshi Yang and Anette M{\"u}llertz and Ren{\'e} Holm and Huiling Mu",
year = "2017",
month = "9",
doi = "10.1111/jphp.12758",
language = "English",
volume = "69",
pages = "1110--1115",
journal = "Journal of Pharmacy and Pharmacology",
issn = "0022-3573",
publisher = "JohnWiley & Sons Ltd",
number = "9",

}

RIS

TY - JOUR

T1 - Efficacy of oral lipid-based formulations of apomorphine and its diester in a Parkinson's disease rat model

AU - Borkar, Nrupa

AU - Andersson, Daniel R.

AU - Yang, Mingshi

AU - Müllertz, Anette

AU - Holm, René

AU - Mu, Huiling

PY - 2017/9

Y1 - 2017/9

N2 - ObjectivesApomorphine is used to symptomatically treat Parkinson's disease (PD). Oral delivery of apomorphine is generally limited by its short plasma half-life and a hepatic first-pass metabolism. This study was aimed at evaluating the behavioural response of apomorphine and its prodrug administered in oral lipid-based formulations.MethodsThe behavioural response of apomorphine and its prodrug administered in oral lipid-based formulations was evaluated using a 6-hydroxydopamine-lesioned rat model simulating PD symptomatology. Apomorphine or dipalmitoyl apomorphine (DPA) was incorporated into different lipid-based formulations and orally administered (0.24 mmol/kg) to the PD rat model. The rotations by the rats were counted.Key findingsThe duration of response lasted to about 2.5 h with oral apomorphine- and DPA-loaded o/w emulsion, while it was increased to 6 h when DPA was incorporated in self-emulsifying drug delivery systems compared to s.c. apomorphine (1 h). This suggests that the lipid-based formulations provide a sustained drug release allowing for a steady exposure to the brain.ConclusionsOral lipid-based apomorphine delivery has a potential in achieving a steady response, though at a higher dose possibly eliminating the need for frequent s.c. apomorphine administration.

AB - ObjectivesApomorphine is used to symptomatically treat Parkinson's disease (PD). Oral delivery of apomorphine is generally limited by its short plasma half-life and a hepatic first-pass metabolism. This study was aimed at evaluating the behavioural response of apomorphine and its prodrug administered in oral lipid-based formulations.MethodsThe behavioural response of apomorphine and its prodrug administered in oral lipid-based formulations was evaluated using a 6-hydroxydopamine-lesioned rat model simulating PD symptomatology. Apomorphine or dipalmitoyl apomorphine (DPA) was incorporated into different lipid-based formulations and orally administered (0.24 mmol/kg) to the PD rat model. The rotations by the rats were counted.Key findingsThe duration of response lasted to about 2.5 h with oral apomorphine- and DPA-loaded o/w emulsion, while it was increased to 6 h when DPA was incorporated in self-emulsifying drug delivery systems compared to s.c. apomorphine (1 h). This suggests that the lipid-based formulations provide a sustained drug release allowing for a steady exposure to the brain.ConclusionsOral lipid-based apomorphine delivery has a potential in achieving a steady response, though at a higher dose possibly eliminating the need for frequent s.c. apomorphine administration.

U2 - 10.1111/jphp.12758

DO - 10.1111/jphp.12758

M3 - Journal article

C2 - 28620913

VL - 69

SP - 1110

EP - 1115

JO - Journal of Pharmacy and Pharmacology

JF - Journal of Pharmacy and Pharmacology

SN - 0022-3573

IS - 9

ER -

ID: 183728446