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. 2016 Jun 28;7:185. doi: 10.3389/fphar.2016.00185
(1) Particle size
Drug loading and release rates from PLGA particles do not necessarily conform to predicted behavior as the effect of microparticle size on drug release kinetics quantitatively can only be predicted for certain well-defined formulations.
Encapsulated drug Particle size (μm) Drug loading or EE Drug release profile References
Lidocaine Increase from 20 to 50 to 120 N/A Release rate ↓ as particle size ↑ Klose et al., 2006
Huperzine A Increase from 125–200 to 200–400 to 400–700 EE ↑ Release rate ↓ as particle size ↑ Fu et al., 2005
Dexamethasone 1.0 11% Slow-release particles but with initial burst release Dawes et al., 2009
20 1% Sustained release over a 550 h period
5-fluorouracil 70–120 35% ~90% release in 7 days Siepmann et al., 2004
20 20% 90% release over 21days
Drug-free < 50, < 20 and < 1 (each size prepared by a different process) N/A At pH 7.4 and 37°C, ↑ polymer degradation rate for larger microspheres Dunne et al., 2000