TY - JOUR
T1 - Quercetin Liposomal Nanoformulation for Ischemia and Reperfusion Injury Treatment
AU - Ferreira‐silva, Margarida
AU - Faria‐silva, Catarina
AU - Carvalheiro, Manuela C.
AU - Simões, Sandra
AU - Marinho, H. Susana
AU - Marcelino, Paulo
AU - Campos, Maria Celeste
AU - Metselaar, Josbert M.
AU - Fernandes, Eduarda
AU - Baptista, Pedro V.
AU - Fernandes, Alexandra R.
AU - Corvo, M. Luísa
N1 - PD/BD/135264/2017
UID/DTP/04138/2020
UIDP/04138/2020
UIDP/04378/2020
UIDB/04378/2020
LA/P/0140/2020
UIDB/50006/2020
UIDB/00100/2020
PY - 2022/1/3
Y1 - 2022/1/3
N2 - Ischemia and reperfusion injury (IRI) is a common complication caused by inflammation and oxidative stress resulting from liver surgery. Current therapeutic strategies do not present the desirable efficacy, and severe side effects can occur. To overcome these drawbacks, new therapeutic alternatives are necessary. Drug delivery nanosystems have been explored due to their capacity to improve the therapeutic index of conventional drugs. Within nanocarriers, liposomes are one of the most successful, with several formulations currently in the market. As improved therapeutic outcomes have been demonstrated by using liposomes as drug carriers, this nanosystem was used to deliver quercetin, a flavonoid with anti-inflammatory and antioxidant properties, in hepatic IRI treatment. In the present work, a stable quercetin liposomal formulation was developed and characterized. Additionally, an in vitro model of ischemia and reperfusion was developed with a hypoxia chamber, where the anti-inflammatory potential of liposomal quercetin was evaluated, revealing the downregulation of pro-inflammatory markers. The anti-inflammatory effect of quercetin liposomes was also assessed in vivo in a rat model of hepatic IRI, in which a decrease in inflammation markers and enhanced recovery were observed. These results demonstrate that quercetin liposomes may provide a significant tool for addressing the current bottlenecks in hepatic IRI treatment.
AB - Ischemia and reperfusion injury (IRI) is a common complication caused by inflammation and oxidative stress resulting from liver surgery. Current therapeutic strategies do not present the desirable efficacy, and severe side effects can occur. To overcome these drawbacks, new therapeutic alternatives are necessary. Drug delivery nanosystems have been explored due to their capacity to improve the therapeutic index of conventional drugs. Within nanocarriers, liposomes are one of the most successful, with several formulations currently in the market. As improved therapeutic outcomes have been demonstrated by using liposomes as drug carriers, this nanosystem was used to deliver quercetin, a flavonoid with anti-inflammatory and antioxidant properties, in hepatic IRI treatment. In the present work, a stable quercetin liposomal formulation was developed and characterized. Additionally, an in vitro model of ischemia and reperfusion was developed with a hypoxia chamber, where the anti-inflammatory potential of liposomal quercetin was evaluated, revealing the downregulation of pro-inflammatory markers. The anti-inflammatory effect of quercetin liposomes was also assessed in vivo in a rat model of hepatic IRI, in which a decrease in inflammation markers and enhanced recovery were observed. These results demonstrate that quercetin liposomes may provide a significant tool for addressing the current bottlenecks in hepatic IRI treatment.
KW - Anti-inflammatory therapy
KW - Drug delivery nanosystems
KW - Hepatic ischemia and reperfusion injury
KW - Inflammation
KW - Liposomes
KW - Liver
KW - Quercetin
UR - http://www.scopus.com/inward/record.url?scp=85122158350&partnerID=8YFLogxK
U2 - 10.3390/pharmaceutics14010104
DO - 10.3390/pharmaceutics14010104
M3 - Article
C2 - 35057000
AN - SCOPUS:85122158350
SN - 1999-4923
VL - 14
JO - Pharmaceutics
JF - Pharmaceutics
IS - 1
M1 - 104
ER -