Preparation of DHAQ-loaded mPEG-PLGA-mPEG nanoparticles and evaluation of drug release behaviors in vitro/in vivo

  • Yourong Duan
  • Xun Sun
  • Tao Gong
  • Qi Wang
  • Zhirong Zhang


This study describes the preparation and the evaluation of biodegradation monomethoxy (polyethylene glycol)-poly (lactide-co-glycolide)-monomethoxy (polyethyleneglycol) (mPEG-PLGA-mPEG, PELGE) nanoparticles (PELGE-NP) containing mitoxantrone (DHAQ) as a model drug. PELGE copolymers with various molar ratios of lactic to glycolic acid and different molecular weights and various content mPEG were synthesized by ring-opening polymerization. mPEG with weight-average molecular weight (Mw) 2000 or 5000 was introduced as a hydrophilic segment into a hydrophobic PLGA. A double emulsion method with dextran70 as stabilizer in the external aqueous phase was used to prepare the nanoparticles. The drug entrapment efficiencies were more than 80% and the mean diameters of the nanoparticles were less than 200 nm. Various PELGE was studied as biodegradable drug carriers and there in vitro/in vivo release profiles were examined. It was found that drug loading, polymer molecular weight, copolymer composition and end group modifications were critical factors affecting the in vitro/in vivo release properties. The amount of drug released increased as the mPEG contents increased and the molar ratios of lactic acid decreased in vitro. The intravenous (i.v.) administration of mPEG-PLGA–mPEG nanoparticles of DHAQ in mice resulted in prolonged DHAQ residence in systemic blood circulation compared to the intravenous administration of PLGA nanoparticles.


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  1. 1.
    Y. I. JEONG and J. W. NAH, J. Appl. Polym. Sci. 80 (2001) 2228.CrossRefGoogle Scholar
  2. 2.
  3. 3.
    S. M. LI, in Degradable Polymers: Principles and Applications (Chapman and Hall, London, 1995) p. 43.Google Scholar
  4. 4.
    R. GREF and A. DOMB, Adv. Drug. Deliv. Rev. 16 (1995) 215.CrossRefGoogle Scholar
  5. 5.
    N. V. MAJETI and R. KUMAR, J. Pharm. Pharmaceut. Sci. 3 (2000) 234.Google Scholar
  6. 6.
    K. AVGOUSTAKIS and D. S. ITHAKISSIOS, J. Contr. Rel. 79 (2002) 123.CrossRefGoogle Scholar
  7. 7.
    E. CHIOTELIS and J. G. MCAFEE, Int. J. Nucl. Med. Biol. 4 (1977) 29.CrossRefGoogle Scholar
  8. 8.
    G. SPENLEHAUER and J. P. BENOIT, Biomaterials 10 (1989) 557.CrossRefGoogle Scholar
  9. 9.
    R. H. MULLER and O. KAYSER, Adv. Drug. Deliv. Rev. 47 (2001) 3.CrossRefGoogle Scholar
  10. 10.
    M. L. HANS and A. M. LOWMAN, Curr. Opin. Solid State Mat. Sci. 6 (2002) 319.CrossRefGoogle Scholar
  11. 11.
    T. REIHS and M. MULLER, J. Colloid. Interface Sci. 271 (2004) 69.CrossRefGoogle Scholar
  12. 12.
    A. J. RAJEEV, Biomaterials 21 (2000) 2475.CrossRefGoogle Scholar
  13. 13.
    R. GREF and R. LANGER, Science 263 (1994) 1600.Google Scholar
  14. 14.
    H. FESSI and S. BENITA, Int. J. Pharm. 55 (1989) R1.CrossRefGoogle Scholar
  15. 15.
    J. W. FONG and H. V. MAULDING, J. Contr. Rel. 3 (1986) 119.CrossRefGoogle Scholar
  16. 16.
    D. BAZILE and M. VEILLARD, J. Pharm. Sci. 84 (1995) 493.Google Scholar
  17. 17.
    J. W. NAH and C. S. CHO, J. Polym. Sci. B : Polym. Phys. 36 (1998) 415.CrossRefGoogle Scholar
  18. 18.
    M. VITTAZ and G. SENLEHAUER, Biomaterials 17 (1996) 1575.CrossRefGoogle Scholar

Copyright information

© Springer Science + Business Media, LLC 2006

Authors and Affiliations

  • Yourong Duan
    • 1
  • Xun Sun
    • 2
  • Tao Gong
    • 2
  • Qi Wang
    • 2
  • Zhirong Zhang
    • 2
  1. 1.Shanghai Cancer InstituteCancer Institute of Shanghai JiaoTong UniversityShanghaiChina
  2. 2.West China School of PharmacySichuan UniversityChengduChina

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