Chitosan-coated liposomes loaded with butyric acid demonstrate anticancer and anti-inflammatory activity in human hepatoma HepG2 cells

Vincenzo Quagliariello, Mario Masarone, Emilia Armenia, Aldo Giudice, Manlio Barbarisi, Michele Caraglia, Alfonso Barbarisi, Marcello Persico

Research output: Contribution to journalArticlepeer-review

Abstract

Butyric acid (BA) has been reported to induce anticancer effects on hepatocellular carcinoma (HCC) cells both in vitro and in vivo. However, its delivery and release in cancer tissues must be optimized. On the basis of these requirements, we prepared liposomes coated with chitosan and uncoated liposomes and both types were loaded with BA through a thin-film hydration method. The liposomes coated or uncoated with chitosan had a mean hydrodynamic size of 83.5 and 110.3 nm, respectively, with a homogeneous size distribution of the particles. For evaluation of the biological effects of the nanoformulations, the hepatoblastoma (HB) HepG2 cell line was utilized. BA-loaded liposomes coated with chitosan showed a considerable higher cytotoxicity than both uncoated liposomes and free BA, with IC50 values, after 72 h of incubation, of 7.5, 2.5 and 1.6 mM, respectively. Treatment of HepG2 cells for 5 h with the BA-loaded liposomes coated with chitosan at 5 mM lowered the extent of the increase in IL-8, IL-6, TNF-α and TGF-β expression of approximately 64, 58, 85 and 73.8%, respectively, when compared to the untreated cells. The BA-loaded liposomes coated with chitosan had marked capacity to be internalized in human HB cells showing an increased cytotoxic activity when compared with free BA and important anti-inflammatory effects by inhibiting production of cytokines with a central role in liver cell survival.

Original languageEnglish
Pages (from-to)1476-1486
Number of pages11
JournalOncology Reports
Volume41
Issue number3
DOIs
Publication statusPublished - Mar 1 2019

Keywords

  • Butyric acid
  • Cytokines
  • Inflammation
  • Liposome
  • Liver cells

ASJC Scopus subject areas

  • Oncology
  • Cancer Research

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