The modulation of physicochemical characterization of innovative liposomal platforms: the role of the grafted thermoresponsive polymers

Pharm Dev Technol. 2017 May;22(3):330-335. doi: 10.3109/10837450.2015.1121497. Epub 2015 Dec 7.

Abstract

This study is focused on chimeric advanced drug delivery systems and specifically on thermosensitive liposomes, combining lipids and thermoresponsive polymers. In this investigation, 1,2-dipalmitoyl-sn-glycero-3-phosphocholine (DPPC) chimeric liposomal systems were prepared, incorporating the homopolymer C12H25-poly(N-isopropylacrylamide)-COOH (C12H25-PNIPAM-COOH) and the block copolymer poly(n-butylacrylate-b-N-isoropylacrylamide) (PnBA-PNIPAM), at six different molar ratios. Both of these polymers contain the thermoresponsive PNIPAM block, which exhibits lower critical solution temperature (LCST) at 32 °C in aqueous solutions, changing its nature from hydrophilic to hydrophobic above LCST. During the preparation of liposomes, the dispersions were observed visually, while after the preparation we studied the alterations of the physicochemical characteristics, by measuring the size, size distribution and ζ-potential of prepared liposomes. The presence of polymer, either C12H25-PNIPAM-COOH or PnBA-PNIPAM, resulted in liposomes exhibiting different physicochemical characteristics in comparison to conventional DPPC liposomes. At the highest percentage of the polymeric guest, chimeric liposomes were found to retain their size during the stability studies. The incorporation of the appropriate amount of these novel thermoresponsive polymers yields liposomal stabilization and imparts thermoresponsiveness, due to the functional PNIPAM block.

Keywords: Chimeric advanced drug delivery systems; lipids; thermoresponsive polymers; thermosensitive liposomes.

MeSH terms

  • 1,2-Dipalmitoylphosphatidylcholine / chemistry*
  • Acrylates / chemistry*
  • Acrylic Resins / chemistry*
  • Chemical Phenomena
  • Hot Temperature
  • Hydrophobic and Hydrophilic Interactions
  • Liposomes / chemistry*
  • Particle Size
  • Polymers / chemistry*
  • Technology, Pharmaceutical / methods*

Substances

  • Acrylates
  • Acrylic Resins
  • Liposomes
  • Polymers
  • poly(n-butyl acrylate)
  • poly-N-isopropylacrylamide
  • 1,2-Dipalmitoylphosphatidylcholine