Abstract:
:PLGA microspheres undergo physical ageing but their ageing kinetics have not been reported, nor the effect of encapsulated protein or plasmid DNA on any associated changes to the glass transition. Differential scanning calorimetry (DSC) was used to measure the rate of ageing of various PLGA microsphere formulations, with temperature-modulated DSC used to accurately measure the associated glass transition. The Cowie-Ferguson model was applied to determine the parameters describing the enthalpy relaxation kinetics. We show that encapsulated proteins had no significant effect on the glass transition of the microspheres, whereas DNA and PVA were mild antiplasticising agents, particularly with high Mw PLGA. Physical ageing occurred through a range of enthalpy relaxation times (or modes) and was independent of both encapsulated protein and surfactant used during microsphere preparation. Analysis of accelerated ageing at 35 degrees C gave calculated enthalpy relaxation times to thermal equilibrium of 280-400 h. No ageing was observed < or = 10 degrees C and at 25 degrees C estimated relaxation times were at least one order of magnitude greater than at 35 degrees C. Ageing of PLGA microspheres therefore occurs at temperatures >10 degrees C, but relaxation will be far from equilibrium unless storage times and/or temperatures are prolonged or nearing the glass transition, respectively.
journal_name
Int J Pharmjournal_title
International journal of pharmaceuticsauthors
Rouse JJ,Mohamed F,van der Walle CFdoi
10.1016/j.ijpharm.2007.02.026subject
Has Abstractpub_date
2007-07-18 00:00:00pages
112-20issue
1-2eissn
0378-5173issn
1873-3476pii
S0378-5173(07)00199-8journal_volume
339pub_type
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