PLGA microparticles with zero-order release of the labile anti-Parkinson drug apomorphine.

Abstract:

:The treatment of patients suffering from advanced Parkinson's disease is highly challenging, because the efficacy of the "gold standard" levodopa declines with time. Co-administration of the dopamine receptor agonist apomorphine is beneficial, but difficult due to the poor oral bioavailability and short half-life of this drug. In order to overcome these restrictions, PLGA-based microparticles allowing for controlled parenteral delivery of this morphine derivative were prepared using (solid-in-)oil-in-water extraction/evaporation techniques. Particular attention was paid to minimize spontaneous oxidation of the labile drug and to optimize the key features of the microparticles, including encapsulation efficiency, initial burst release and particle size. Various formulation and processing parameters were adjusted in this respect. The systems were thoroughly characterized using SEM, EDX, DSC, laser diffraction, headspace-GC as well as in vitro drug release measurements in agitated flasks and flow-through cells. Importantly, apomorphine could effectively be protected against degradation during microparticle preparation and within the delivery systems upon exposure to phosphate buffer pH 7.4 (containing 0.2% ascorbic acid) at 37 °C: 90% intact drug was released at a constant rate during about 10d.

journal_name

Int J Pharm

authors

Regnier-Delplace C,Thillaye du Boullay O,Siepmann F,Martin-Vaca B,Degrave N,Demonchaux P,Jentzer O,Bourissou D,Siepmann J

doi

10.1016/j.ijpharm.2013.01.008

subject

Has Abstract

pub_date

2013-02-25 00:00:00

pages

68-79

issue

1-2

eissn

0378-5173

issn

1873-3476

pii

S0378-5173(13)00021-5

journal_volume

443

pub_type

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