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Evaluation ofin vitro release profiles of fentanyl-loaded PLGA oligomer microspheres

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Abstract

In order to the development of the delivery device of long-acting local anesthetics for postoperative analgesia and control of chronic pain of cancer patient, fentanyl-loaded poly(l-lactide-co-glycolide)|(PLGA, molecular weight, 5,000 g/mole; 50∶50 mole ratio by lactide to glycolide)|microspheres (FMS)|were studied. FMS were prepared by an emulsion solvent-evaporation method. The influence of several preparation parameters such as initial drug loading, PLGA concentration, emulsifier concentration, oil phase volume, and fabrication temperature has been investigated on the fentanyl release profiles. Generally, the drug showed the biphasic release patterns, with an initial diffusion followed by a lag period before the onset of the degradation phase, but there was no lag time in our system. Fentanyl was slowly released from FMS over 10 daysin vitro with a quasi-zero order property. The release rate increased with increasing drug loading as well as decreasing polymer concentration with relatively small initial burst effect. From the results, FMS may be a good formulation to deliver the anesthetic for the treatment of chronic pain.

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References

  1. R. C. Baselt,Disposition of Toxic Drugs and Chemicals in Man, 2nd Eds., Davis, Ed., Biomedical Publications, 1982, pp 325.

  2. W. R. Hammargren and G. L. Henderson,J. Anal. Toxicol.,12, 183 (1988).

    CAS  Google Scholar 

  3. B. E. Marchall and D. E. Longnecker,General Anesthetics, A. G. Gilman, T. W. Rall, A. S. Nies, and P. Taylor, Eds., Pegamon Press, New York, 1990, pp 305–327.

    Google Scholar 

  4. J. C. Garriott, R. Rodriquez, and V. J. M. Di Mario,J. Anal. Toxicol.,8, 288 (1984).

    CAS  Google Scholar 

  5. (5)E. M. Pare, J. R. Monforte, R. Gaul, and H. Mirchandani,J. Anal. Toxicol.,11, 272 (1987).

    CAS  Google Scholar 

  6. R. J. Matecjczyk,J. Anal. Toxicol.,12, 236 (1988).

    Google Scholar 

  7. B. Levine, J. C. Goodin, and Y. H. Caplan,Forensic Sci. Int.,45, 247 (1990).

    Article  CAS  Google Scholar 

  8. H. S. Choi, H. C. Shin, G. Khang, J. M. Rhee and H. B. Lee,J. Chromatography B.,765, 63 (2001).

    Article  CAS  Google Scholar 

  9. H. S. Choi, S.-A. Seo, G. Khang. J. M. Rhee, and H. B. Lee,Int. J. Pharm.,234, 195 (2002).

    Article  CAS  Google Scholar 

  10. S. -A. Seo, H. S. Choi, G. Khang, J. M. Rhee, and H. B. Lee,Int. J. Pharm.,239, 93 (2002).

    Article  CAS  Google Scholar 

  11. L. R. Beck, V. Z. Pope, T. R. Tice, and R. M. Gilley,Adv. Contracept.,1, 19 (1985).

    Article  Google Scholar 

  12. A. C. Moffat, inClarke’s Isolation, Identification of Drugs in Pharmaceuticals, Body Fluids and Post-Mortem Materials, Pharmaceutical Press, London, 1986, pp 617–638.

    Google Scholar 

  13. R. Ikeda and C. Pelton,J. Med.,152, 617 (1990).

    CAS  Google Scholar 

  14. H. B. Lee, G. Khang, J. C. Cho, J. M. Rhee, and J. S. Lee,Polymer Preprints,40, 288 (1999).

    CAS  Google Scholar 

  15. G. Khang, J. M. Rhee, J. S. Lee, and H. B. Lee,Polymer Sci. Tech.,12, 4 (2001).

    CAS  Google Scholar 

  16. G. Khang, D. S. Moon, H. S. Seong, J. M. Rhee, J. S. Lee, and H. B. Lee,Biomater. Res.,4, 107 (2000).

    Google Scholar 

  17. J. C. Cho, G. Khang, J. M. Rhee, Y. S. Kim, J. S. Lee, and H. B. Lee,Korea Polym. J.,7, 79 (1999).

    CAS  Google Scholar 

  18. G. Khang, J. C. Cho, J. W. Lee, J. M. Rhee, and H. B. Lee,Bio-Med. Mater. Eng.,9, 49 (1999).

    CAS  Google Scholar 

  19. G. Khang, J. H. Lee, J. W. Lee, J. C. Cho, and H. B. Lee,Korea Polym. J.,8, 80 (2000).

    CAS  Google Scholar 

  20. J. C. Cho, G. Khang, H. S. Choi, J. M. Rhee, S. C. Yoon, J. C. Cho, and H. B. Lee,Polymer (Korea),24, 728 (2000).

    CAS  Google Scholar 

  21. G. Khang, H. S. Choi, J. M. Rhee, S. C. Yoon, J. C. Cho, and H. B. Lee,Korea Polym. J.,8, 253 (2000).

    Google Scholar 

  22. W.-I. Son, D. I. Yun, G. Khang, B.-S. Kim, and, H. B. Lee,Biomater. Res.,4, 92 (2000).

    Google Scholar 

  23. J. C. Cho, G. Khang, J. M. Rhee, Y. S. Kim, J. S. Lee, and H. B. Lee,Biomater. Res.,4, 136 (2000).

    Google Scholar 

  24. G. Khang, S. W. Kim, J. C. Cho, J. M. Rhee, S. C. Yoon, and H. B. Lee,Bio-Med. Mater. Eng.,11, 89 (2001).

    CAS  Google Scholar 

  25. M. K. Choi, G. Khang, I. Lee, J. M. Rhee, and H. B. Lee,Polymer (Korea),25, 318 (2001).

    CAS  Google Scholar 

  26. S.-A. Seo, H. S. Choi, D. H. Lee, G. Khang, J. M. Rhee, and H. B. Lee,Polymer (Korea),25, 884 (2001).

    CAS  Google Scholar 

  27. S.-A. Seo, H. S. Choi, J. C. Cho, G. Khang, J. M. Rhee, and H. B. Lee,Biomater. Res.,5, 35 (2001).

    Google Scholar 

  28. S. J. Lee, G. Khang, Y. M. Lee, and H. B. Lee,J. Biomater. Sci., Polym. Ed.,13, 197 (2002).

    Article  CAS  Google Scholar 

  29. G. Khang and H. B. Lee, inCell-synthetic Surface Interaction: Physicochemical Surface Modification, A. Atala and R. Lanza, Eds., Academic Press, London, 2001, Section II, pp 771–797.

    Google Scholar 

  30. G. Khang and H. B. Lee,Biomedical Polymer, Korea Chemical Society Press, Munundang, Seoul, Korea, 2001.

    Google Scholar 

  31. D. H. Lewis, inControlled Release of Bioactive Agents from Lactide/Glycolide Polymers, Biodegradable Polymers as Drug Delivery Systems, M. Chasin and R. Langer, Eds., Academic Press, New York, 1990, pp 1–41.

    Google Scholar 

  32. R. Arshady,J. Bioact. Compatible Polym.,5, 315 (1990).

    Article  CAS  Google Scholar 

  33. R. Jalil and J. R. Nixon,J. Microencapsul.,7, 297 (1990).

    Article  CAS  Google Scholar 

  34. R. Jalil and J. R. Nixon,J. Microencapsul.,7, 53 (1990). (35)|Y.-Y. Yang, T.-S. Chung, and N. P. Ng,Biomaterials,22, 231 (2001).

    Article  CAS  Google Scholar 

  35. C. Sturesson, J. Carlfores, K. Edman, and M. Andersson,Int. J. Pharm.,89, 235 (1993).

    Article  CAS  Google Scholar 

  36. M. Guyot and F. Fawaz,Int. J. Pharm.,175, 61 (1998).

    Article  CAS  Google Scholar 

  37. R. Jalil and J. R. Nixon,J. Microencapsul.,7, 245 (1990). (39)|R. Jalil and J. R. Nixon,J. Microencapsul.,7, 41 (1990).

    Article  CAS  Google Scholar 

  38. F. Wada, S. Hyon, and Y. Ikada,J. Pharm. Pharmacol.,43, 605 (1991).

    Article  CAS  Google Scholar 

  39. G. Raouf, S. Cecilia, and C. Johan, Int. J. Pharm.,141, 205 (1996).

    Article  Google Scholar 

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Authors and Affiliations

  1. Department of Polymer Science and Technology, Chonbuk National University, 664-14 Dukjin, 561-756, Chonju, Korea

    Gilson Khang, Sun-Ah Seo, Hak Soo Choi & John M. Rhee

  2. Biomaterials Laboratory, Korea Research Institute of Chemical Technology, Yusung, P. O. Box 107, 305-606, Taejon, Korea

    Hai Bang Lee

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  1. Gilson Khang
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  2. Sun-Ah Seo
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  4. John M. Rhee
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Khang, G., Seo, SA., Choi, H.S. et al. Evaluation ofin vitro release profiles of fentanyl-loaded PLGA oligomer microspheres. Macromol. Res. 10, 246–252 (2002). https://doi.org/10.1007/BF03218313

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  • DOI: https://doi.org/10.1007/BF03218313

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