Efficacy of oral lipid-based formulations of apomorphine and its diester in a Parkinson's disease rat model
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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 journal › Journal article › Research › peer-review
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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