Bulletin of the Korean Chemical Society

Korean Chemical Society (대한화학회)
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Development of Drug-Loaded PLGA Microparticles with Different Release Patterns for Prolonged Drug Delivery

  • Choi, Yeon-Soon (Department of Chemistry, College of Natural Science, Seoul National University) ;
  • Joo, Jae-Ryang (Department of Chemistry, College of Natural Science, Seoul National University) ;
  • Hong, Areum (Department of Chemistry, College of Natural Science, Seoul National University) ;
  • Park, Jong-Sang (Department of Chemistry, College of Natural Science, Seoul National University)
  • Received : 2010.11.29
  • Accepted : 2011.01.04
  • Published : 2011.03.20
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Abstract

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 $48.02{\mu}m$ to $10.63{\mu}m$) 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.

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References

  1. Choi, H. S.; Seo, S. A.; Khang, G.; Rhee, J. M.; Lee, H. B. Int. J. Pharm. 2002, 234, 195. https://doi.org/10.1016/S0378-5173(01)00968-1
  2. Xie, S.; Wang, S.; Zhu, L.; Wang, F.; Zhour, W. Colloid. Surface B 2009, 74, 358. https://doi.org/10.1016/j.colsurfb.2009.08.005
  3. Lee, W. K.; Park, J. Y.; Yang, E. H.; Suh, H.; Kim, S. H.; Chung, D. S.; Choi, K.; Yang, C. W.; Park, J. S. J. Control. Release 2002, 84, 115. https://doi.org/10.1016/S0168-3659(02)00239-0
  4. Berkland, C.; Kim, K.; Pack, D. W. J. Control. Release 2001, 73, 59. https://doi.org/10.1016/S0168-3659(01)00289-9
  5. Govender, T.; Stolnik, S.; Garnett, M. C.; Illum, L.; Davis, S. S. J. Control. Release 1999, 57, 171. https://doi.org/10.1016/S0168-3659(98)00116-3
  6. Ye, M.; Kim, S.; Park, K. J. Control. Release 2010, 146, 241. https://doi.org/10.1016/j.jconrel.2010.05.011
  7. Freitas, S.; Merkle, H. P.; Gander, B. J. Control. Release 2005, 102, 313. https://doi.org/10.1016/j.jconrel.2004.10.015
  8. Katou, H.; Wandrey, A. J.; Gander, B. Int. J. Pharm. 2008, 364, 45. https://doi.org/10.1016/j.ijpharm.2008.08.015
  9. Yeo, Y.; Park, K. Arch. Pharm. Res. 2004, 27, 1. https://doi.org/10.1007/BF02980037
  10. Yang, Y.; Chung, T.; Ng, N. P. Biomaterials 2001, 22, 231. https://doi.org/10.1016/S0142-9612(00)00178-2
  11. Berkland, C.; King, M.; Cox, A.; Kim, K.; Pack, D. W. J. Control. Release 2002, 82, 137. https://doi.org/10.1016/S0168-3659(02)00136-0

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