Phospholipid-Block Copolymer Hybrid Vesicles with Lysosomal Escape Ability

Research output: Contribution to journal/Conference contribution in journal/Contribution to newspaperJournal articleResearchpeer-review

  • Wei Zong
  • ,
  • Bo Thingholm
  • ,
  • Fabian Itel
  • ,
  • Philipp S. Schattling
  • ,
  • Edit Brodszkij
  • Daniel Mayer, University Hospital of Ulm
  • ,
  • Steffen Stenger, University Hospital of Ulm
  • ,
  • Kenneth N. Goldie, University of Basel
  • ,
  • Xiaojun Han, State Key Laboratory of Urban Water Resource and Environment, Harbin Institute of Technology
  • ,
  • Brigitte Städler

The success of nanoparticulate formulations in drug delivery depends on various aspects including their toxicity, internalization, and intracellular location. Vesicular assemblies consisting of phospholipids and amphiphilic block copolymers are an emerging platform, which combines the benefits from liposomes and polymersomes while overcoming their challenges. We report the synthesis of poly(cholesteryl methacrylate)-block-poly(2-(dimethylamino) ethyl methacrylate) (pCMA-b-pDMAEMA) block copolymers and their assembly with phospholipids into hybrid vesicles. Their geometry, their ζ-potential, and their ability to adsorb onto polymer-coated surfaces were assessed. Giant unilamellar vesicles were employed to confirm the presence of both the phospholipids and the block copolymer in the same membrane. Furthermore, the cytotoxicity of selected hybrid vesicles was determined in RAW 264.7 mouse macrophages, primary rat Kupffer cells, and human macrophages. The internalization and lysosomal escape ability of the hybrid vesicles were confirmed using RAW 264.7 mouse macrophages. Taken together, our findings illustrate that the reported hybrid vesicles are a promising complementary drug delivery platform for existing liposomes and polymersomes.

Original languageEnglish
Pages (from-to)6874-6886
Number of pages13
Publication statusPublished - 12 Jun 2018

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