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

Research output: Contribution to journalArticlepeer-review

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 nano-structured 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 ring-opening 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
Pages (from-to)6725-6736
Number of pages12
JournalJournal of Nanoparticle Research
Volume13
Issue number12
DOIs
Publication statusPublished - 25 Sept 2011

Keywords

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

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