Bombesin receptor-targeted liposomes for enhanced delivery to lung cancer cells

Mohammad Akbar, Pamela Lukasewicz Ferreira, Melania Giorgetti, Leanne Stokes, Christopher Morris

Research output: Contribution to journalArticlepeer-review

8 Citations (Scopus)
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Background: Gastrin-releasing peptide is a member of the bombesin family of peptides. Its cognate receptor, GRPR, is widely expressed in cancers of the lung, pancreas and ovaries. GRP is an autocrine growth factor in small cell lung cancer, which has very poor patient outcomes. High affinity antagonist peptides have been developed for in vivo cancer imaging. In this report we decorated pegylated liposomes with a GRPR antagonist peptide and studied its interaction with and accumulation within lung cancer cells.
Results: An N-terminally cysteine modified GRPR antagonist (termed cystabn) was synthesised and shown to inhibit cell growth in vitro. Cystabn was used to prepare a targeted 1,2-distearoyl-sn-glycero-3-phosphoethanolamine-N-[amino(polyethylene glycol)-2000] (DSPE-PEG2000) lipid conjugate that was formulated into liposomes. The liposomes displayed desirable colloidal properties and good stability under storage conditions. Flow cytometric and microscopic studies showed that fluorescently labelled cystabn-decorated liposomes accumulated more extensively in GRPR over-expressing cells than matched liposomes that contained no cystabn targeting motif.
Conclusion: The use of GRPR antagonistic peptides for nanoparticle targeting has potential for enhancing drug accumulation in resistant cancer cells.
Original languageEnglish
Pages (from-to)2553–2562
Number of pages10
JournalBeilstein journal of Nanotechnology
Publication statusPublished - 19 Dec 2019

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