(1) Particle size | ||||
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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 |