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 language | English |
|---|---|
| Pages (from-to) | 1476-1486 |
| Number of pages | 11 |
| Journal | Oncology Reports |
| Volume | 41 |
| Issue number | 3 |
| DOIs | |
| Publication status | Published - Mar 1 2019 |
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Keywords
- Butyric acid
- Cytokines
- Inflammation
- Liposome
- Liver cells
ASJC Scopus subject areas
- Oncology
- Cancer Research
Cite this
Chitosan-coated liposomes loaded with butyric acid demonstrate anticancer and anti-inflammatory activity in human hepatoma HepG2 cells. / Quagliariello, Vincenzo; Masarone, Mario; Armenia, Emilia; Giudice, Aldo; Barbarisi, Manlio; Caraglia, Michele; Barbarisi, Alfonso; Persico, Marcello.
In: Oncology Reports, Vol. 41, No. 3, 01.03.2019, p. 1476-1486.Research output: Contribution to journal › Article
}
TY - JOUR
T1 - Chitosan-coated liposomes loaded with butyric acid demonstrate anticancer and anti-inflammatory activity in human hepatoma HepG2 cells
AU - Quagliariello, Vincenzo
AU - Masarone, Mario
AU - Armenia, Emilia
AU - Giudice, Aldo
AU - Barbarisi, Manlio
AU - Caraglia, Michele
AU - Barbarisi, Alfonso
AU - Persico, Marcello
PY - 2019/3/1
Y1 - 2019/3/1
N2 - 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.
AB - 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.
KW - Butyric acid
KW - Cytokines
KW - Inflammation
KW - Liposome
KW - Liver cells
UR - http://www.scopus.com/inward/record.url?scp=85060809933&partnerID=8YFLogxK
UR - http://www.scopus.com/inward/citedby.url?scp=85060809933&partnerID=8YFLogxK
U2 - 10.3892/or.2018.6932
DO - 10.3892/or.2018.6932
M3 - Article
C2 - 30569138
AN - SCOPUS:85060809933
VL - 41
SP - 1476
EP - 1486
JO - Oncology Reports
JF - Oncology Reports
SN - 1021-335X
IS - 3
ER -