PEGylation and surface functionalization of liposomes containing drug nanocrystals for cell-targeted delivery

Yunxin Xiao, Qingtao Liu, Andrew J. Clulow, Tang Li, Madhura Manohar, Elliot P. Gilbert, Liliana de Campo, Adrian Hawley, B. J. Boyd

Research output: Contribution to journalArticleResearchpeer-review

6 Citations (Scopus)

Abstract

Liposomal formulations have important therapeutic applications in anti-cancer treatments but current formulations suffer from serious side effects, high dosage requirements and prolonged treatment. In this study, PEGylated azide-functionalized liposomes containing drug nanocrystals were investigated with the aim of increasing the drug payload and achieving functionalization for targeted delivery. Liposomes were characterized using cryogenic transmission electron microscopy (cryo-TEM), dynamic light scattering (DLS), small and ultra-small angle neutron scattering (SANS/USANS) and small and wide angle X-ray scattering (SAXS/WAXS). Cryo-TEM experiments revealed the dimensions of the nanocrystal-loaded liposomes and the change of shape from spherical to elongated after the formation of nanocrystals. Results from SANS/USANS experiments confirmed the asymmetric particle shape. SAXS/WAXS experiments confirmed that the crystalline drug only occurred in freeze-thawed samples and correlated with a new unidentified polymorphic form of ciprofloxacin. Using a small molecule dye, dibenzocyclooctyne (DBCO)-cy5, specific conjugation between DBCO groups and surface azide groups on the liposomes was confirmed; this indicates the promise of this system for tumour-targeted delivery.

Original languageEnglish
Article number110362
Number of pages10
JournalColloids and Surfaces B: Biointerfaces
Volume182
DOIs
Publication statusPublished - 1 Oct 2019

Keywords

  • Click chemistry
  • Drug nanocrystals
  • Liposomes
  • PEGylation
  • Scattering
  • Targeted delivery

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