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Bulletin of the Korean Chemical Society (BKCS)

ISSN 0253-2964(Print)
ISSN 1229-5949(Online)
Volume 32, Number 3
BKCSDE 32(3)
March 20, 2011 

Development of Drug-Loaded PLGA Microparticles with Different Release Patterns for Prolonged Drug Delivery
Yeonsoon Choi , Jae ryang Joo, Areum Hong, Jong Sang Park*
Drug delivery system, Biodegradable polymers, PLGA microparticles, Solvent evaporation method
For the prolonged delivery and sustained release rates of low molecular weight drugs, poly(lactic-co-glycolic acid) (PLGA) microparticles containing the drug SKL-2020 have been investigated. On increasing polyvinyl alcohol (PVA) concentration (from 0.2% to 5%), the size of microparticles decreased (from 48.02 μm to 10.63 μm) and more uniform size distribution was noticeable due to the powerful emulsifying ability of PVA. A higher drug loading (from 5% to 20%) caused a larger concentration gradient between 2 phases at the polymer precipitation step; this resulted in decreased encapsulation efficiency (from 34.19% to 25.67%) and a greater initial burst (from 61.71% to 70.05%). SKL-2020-loaded PLGA microparticles prepared with different fabrication conditions exhibited unique release patterns of SKL-2020. High PVA concentration and high drug loading led to an initial burst effect by rapid drug diffusion through the polymer matrix. Since PLGA microparticles enabled the slow release of SKL-2020 over 1 week in vitro and in vivo, more convenient and comfortable treatment could be facilitated with less frequent administration. It is feasible to design a release profile by mixing microparticles that were prepared with different fabrication conditions. By this method, the initial burst could be repressed properly and drug release rate could decrease.
867 - 872
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