Authors: Dunne, Margaret¹; Ramtoola, Zebunnissa²; Corrigan, Owen¹

Source: Journal of Microencapsulation, Volume 26, Number 5, August 2009 , pp. 403-410(8)

Publisher: Informa Healthcare

Abstract:

The release of actives encapsulated in biodegradable poly-lactide-co-glycolide (PLGA)-based microparticles may be diffusion controlled, dependent on polymer degradation, or may occur by a combination of drug diffusion and polymer degradation. This report applies a model, describing combined diffusional and polymer degradation-assisted drug release, to quantify the release of fluphenazine HCl (F-HCl) from PLGA microspheres. Parameters for the release process showed that both the initial drug release phase and the polymer controlled drug release phase were dependent on the F-HCl loading of the microspheres. The percentage drug released in the burst phase and the length of the lag phase were dependent on F-HCl loading. In the degradation controlled release phase, drug release was faster the higher the loading, as shown by the decrease in tmax from 27 to 10 days, as F-HCl loadings increased from 4.2 to 16.6%w/w. The presence of F-HCl was found to catalyse the degradation of PLGA polymer during particle manufacture and during dissolution. When compared to drug free microspheres, F-HCl accelerated PLGA degradation as shown by the ∼5-fold increase in both PLGA degradation rate constant (k) and reduction in tmax.

Keywords: Fluphenazine; modelling release; burst effect; PLGA

Document Type: Research article

DOI: http://dx.doi.org/10.1080/02652040802396575

Affiliations: 1: School of Pharmacy and Pharmaceutical Sciences, University of Dublin, Dublin, Ireland 2: School of Pharmacy, Royal College of Surgeons in Ireland, Dublin, Ireland

Publication date: 2009-08-01

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