New approach in synthesis, characterization and release study of pH-sensitive polymeric micelles, based on PLA-Lys-b-PEGm, conjugated with doxorubicin

E. K. Efthimiadou, C. Tapeinos, P. Bilalis, G. Kordas*

*Corresponding author for this work

Research output: Contribution to journalArticlepeer-review

25 Scopus citations

Abstract

Amphiphilic block copolymers are well established as building blocks for the preparation of micellar drug carriers. The functional polymer micelles possess several advantages, such as high drug efficiency, targeted delivery, and minimized cytotoxicity. The synthesis of block copolymers using nanostructured templates has emerged as a useful and versatile approach for preparing drug carriers. Here, we report the synthesis of a smart polymeric compound of a diblock PLA-Lys-b-PEG copolymer containing doxorubicin. We have synthesized functionalized diblock copolymers, with lysinol, poly(lactide) and monomethoxy poly(ethylene glycol) via thermal ringopening polymerization and a subsequent six-step substitution reaction. A variety of spectroscopic methods were employed here to verify the product of our synthesis. 1H-Nuclear magnetic resonance and Fourier transform infrared studies validated the expected synthesis of copolymers. Doxorubicin is chemically loaded into micelles, and the ex vitro release can be evaluated either in weak acidic or in SBF solution by UV-vis spectroscopy. Dynamic light scattering, thermo gravimetric analysis, and size exclusion chromatography have also been used.

Original languageEnglish (US)
Pages (from-to)6725-6736
Number of pages12
JournalJournal of Nanoparticle Research
Volume13
Issue number12
DOIs
StatePublished - Dec 2011
Externally publishedYes

Bibliographical note

Funding Information:
Acknowledgments We thank the European Research Council (ERC) for financial support of this study under the ‘‘IDEAS’’ project called ‘‘A Novel Nano-container drug carrier for targeted treatment of prostate cancer’’ with the acronym NANOTHERAPY and the reference number: 232959.

Keywords

  • Biodegradable polymeric backbone
  • Breast cancer
  • DLS
  • Doxorubicin
  • Drug delivery
  • Drug loading
  • Drug release
  • Drug targeting
  • EPR effect
  • FT-IR
  • Lysinol
  • NMR
  • Nanomedicine
  • PLA
  • Polymeric micelles
  • Ring opening polymerization
  • mPEG

ASJC Scopus subject areas

  • Bioengineering
  • Atomic and Molecular Physics, and Optics
  • General Chemistry
  • Modeling and Simulation
  • General Materials Science
  • Condensed Matter Physics

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