pH-Promoted Release of a Novel Anti-Tumour Peptide by "Stealth" Liposomes: Effect of Nanocarriers on the Drug Activity in Cis-Platinum Resistant Cancer Cells.

Abstract:

PURPOSE:To evaluate the potential effects of PEGylated pH-sensitive liposomes on the intracellular activity of a new peptide recently characterized as a novel inhibitor of the human thymidylate synthase (hTS) over-expressed in many drug-resistant human cancer cell lines. METHODS:Peptide-loaded pH-sensitive PEGylated (PpHL) and non-PEGylated liposomes (nPpHL) were carefully characterized and delivered to cis-platinum resistant ovarian cancer C13* cells; the influence of the PpHL on the drug intracellular activity was investigated by the Western Blot analysis of proteins involved in the pathway affected by hTS inhibition. RESULTS:Although PpHL and nPpHL showed different sizes, surface hydrophilicities and serum stabilities, both carriers entrapped the drug efficiently and stably demonstrating a pH dependent release; moreover, the different behavior against J774 macrophage cells confirmed the ability of PEGylation in protecting liposomes from the reticuloendothelial system. Comparable effects were instead observed against C13* cells and biochemical data by immunoblot analysis indicated that PEGylated pH-sensitive liposomes do not modify the proteomic profile of the cells, fully preserving the activity of the biomolecule. CONCLUSION:PpHL can be considered as efficient delivery systems for the new promising anti-cancer peptide.

journal_name

Pharm Res

journal_title

Pharmaceutical research

authors

Sacchetti F,Marverti G,D'Arca D,Severi L,Maretti E,Iannuccelli V,Pacifico S,Ponterini G,Costi MP,Leo E

doi

10.1007/s11095-018-2489-z

subject

Has Abstract

pub_date

2018-09-12 00:00:00

pages

206

issue

11

eissn

0724-8741

issn

1573-904X

pii

10.1007/s11095-018-2489-z

journal_volume

35

pub_type

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