Doubly amphiphilic poly(2-oxazoline)s as high-capacity delivery systems for hydrophobic drugs

Robert Luxenhofer, Anita Schulz, Caroline Roques, Shu Li, Tatiana K. Bronich, Elena V. Batrakova, Rainer Jordan, Alexander V. Kabanov

Research output: Contribution to journalArticle

182 Scopus citations

Abstract

Solubilization of highly hydrophobic drugs with carriers that are non-toxic, non-immunogenic and well-defined remains a major obstacle in pharmaceutical sciences. Well-defined amphiphilic di- and triblock copolymers based on poly(2-oxazolines) were prepared and used for the solubilization of Paclitaxel (PTX) and other water-insoluble drugs. Probing the polymer micelles in water with the fluorescence probe pyrene, an unusual high polar microenvironment of the probe was observed. This coincides with an extraordinary large loading capacity for PTX of 45. wt.% active drug in the formulation as well as high water solubility of the resulting formulation. Physicochemical properties of the formulations, ease of preparation and stability upon lyophilization, low toxicity and immunogenicity suggest that poly(2-oxazoline)s are promising candidates for the delivery of highly challenging drugs. Furthermore, we demonstrate that PTX is fully active and provides superior tumor inhibition as compared to the commercial micellar formulation.

Original languageEnglish (US)
Pages (from-to)4972-4979
Number of pages8
JournalBiomaterials
Volume31
Issue number18
DOIs
StatePublished - Jun 2010

Keywords

  • Drug delivery
  • Polymer micelles
  • Polymerization
  • Polyoxazolines
  • Solvatochromism

ASJC Scopus subject areas

  • Bioengineering
  • Ceramics and Composites
  • Biophysics
  • Biomaterials
  • Mechanics of Materials

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  • Cite this

    Luxenhofer, R., Schulz, A., Roques, C., Li, S., Bronich, T. K., Batrakova, E. V., Jordan, R., & Kabanov, A. V. (2010). Doubly amphiphilic poly(2-oxazoline)s as high-capacity delivery systems for hydrophobic drugs. Biomaterials, 31(18), 4972-4979. https://doi.org/10.1016/j.biomaterials.2010.02.057