alexa Biodegradable nanoparticles containing doxorubicin-PLGA conjugate for sustained release.
Materials Science

Materials Science

Journal of Nanomedicine & Nanotechnology

Author(s): Yoo HS, Oh JE, Lee KH, Park TG

Abstract Share this page

Abstract PURPOSE: Doxorubicin was chemically conjugated to a terminal end group of poly(D,L-lactic-co-glycolic acid) [PLGA] and the doxorubicin-PLGA conjugate was formulated into nanoparticles to sustain the release of doxorubicin. METHODS: A hydroxyl terminal group of PLGA was activated by p-nitrophenyl chloroformate and reacted with a primary amine group of doxorubicin for conjugation. The conjugates were fabricated into ca. 300 nm size nanoparticles by a spontaneous emulsion-solvent diffusion method. The amount of released doxorubicin and its PLGA oligomer conjugates was quantitated as a function of time. The cytotoxicity of the released species was determined using a HepG2 cell line. RESULTS: Loading efficiency and loading percentage of doxorubicin-PLGA conjugate within the nanoparticles were 96.6\% and 3.45 (w/w) \%, respectively while those for unconjugated doxorubicin were 6.7\% and 0.26 (w/w) \%, respectively. Both formulation parameters increased dramatically due to the hydrophobically modified doxorubicin by the conjugation of PLGA. The nanoparticles consisting of the conjugate exhibited sustained release over 25 days, whereas those containing unconjugated free doxorubicin showed rapid doxorubicin release in 5 days. A mixture of doxorubicin and its PLGA oligomer conjugates released from the nanoparticles had comparable IC50 value in a HepG2 cell line compared to that of free doxorubicin. Sustained drug release was attributed to the chemical degradation of conjugated PLGA backbone, which permitted water solubilization and subsequent release of doxorubicin conjugated PLGA oligomers into the medium. CONCLUSIONS: The conjugation approach of doxorubicin to PLGA was potentially useful for nanoparticle formulations that require high drug loading and sustained release. The doxorubicin-PLGA oligomer conjugate released in the medium demonstrated a slightly lower cytotoxic activity than free doxorubicin in a HepG2 cell line.
This article was published in Pharm Res and referenced in Journal of Nanomedicine & Nanotechnology

Recommended Conferences

  • Nano Congress for Next Generation
    August 31-September 01, 2017 Brussels,Belgium
  • Graphene & 2D Materials
    September 14-15, 2017 Edinburgh, Scotland
  • Graphene & 2D Materials
    November 6-7, 2017 Frankfurt, Germany
  • World Congress on Nanoscience and Nano Technology
    October 16-17, 2017 Dubai, UAE
  • World Medical Nanotechnology Congress
    October 18-19, 2017 Osaka, Japan
  • Nanoscienceand Molecular Nanotechnology
    Nov 06-08, 2017 Frankfurt, Germany
Peer Reviewed Journals
Make the best use of Scientific Research and information from our 700 + peer reviewed, Open Access Journals
International Conferences 2017-18
Meet Inspiring Speakers and Experts at our 3000+ Global Annual Meetings

Contact Us

© 2008-2017 OMICS International - Open Access Publisher. Best viewed in Mozilla Firefox | Google Chrome | Above IE 7.0 version