Xiangyan Liu1,2, Yang Zhang3, Ling Liu2, Yifeng Pan2, Yu Hu4, Pu Yang5, Mingmei Liao6. 1. Department of Breast Surgery, Xiangya Hospital, Central South University, Changsha, 410008, People's Republic of China. 2. NHC Key Laboratory of Nanobiological Technology, Xiangya Hospital, Central South University, Changsha, 410008, People's Republic of China. 3. Hepatobiliary and Enteric Surgery Center, Xiangya Hospital, Central South University, Changsha, 410008, People's Republic of China. 4. Center for Experimental Medical Research, Third Xiangya Hospital, Central South University, Changsha, 410013, People's Republic of China. 5. Department of Vascular Surgery, Xiangya Hospital, Central South University, Changsha, 410008, People's Republic of China. 6. NHC Key Laboratory of Nanobiological Technology, Xiangya Hospital, Central South University, Changsha, 410008, People's Republic of China. mingmeiliao@csu.edu.cn.
Abstract
BACKGROUND: Quercetin, a pigment (flavonoid) found in many plants and foods, has good effects on protecting liver function but poor solubility and bioavailability in vivo. A drug delivery system can improve the accumulation and bioavailability of quercetin in liver. In this study, we used liposomal nanoparticles to entrap quercetin and evaluated its protective and therapeutic effects on drug-induced liver injury in rats. METHODS: The nanoliposomal quercetin was prepared by a thin film evaporation-high pressure homogenization method and characterized by morphology, particle size and drug content. Acute liver injury was induced in rats by composite factors, including carbon tetrachloride injection, high-fat corn powder intake and ethanol drinking. After pure quercetin or nanoliposomal quercetin treatment, liver function was evaluated by detecting serum levels of glutamic-pyruvic transaminase (GPT), glutamic-oxal acetic transaminase (GOT) and direct bilirubin (DBIL). Histology of injured liver tissues was evaluated by hematoxylin and eosin staining. RESULTS: On histology, liposomal nanoparticles loading quercetin were evenly distributed spherical particles. The nanoliposomal quercetin showed high bioactivity and bioavailability in rat liver and markedly attenuated the liver index and pathologic changes in injured liver tissue. With nanoliposomal quercetin treatment, the serum levels of GPT, GOT and DBIL were significantly better than treated with pure quercetin. Using liposomal nanoparticles to entrap quercetin might be an effective strategy to reduce hepatic injury and protect hepatocytes against damage. CONCLUSION: Liposomal nanoparticles may improve the solubility and bioavailability of quercetin in liver. Furthermore, nanoliposomal quercetin could effectively protect rats against acute liver injury and may be a new hepatoprotective and therapeutic agent for patients with liver diseases.
BACKGROUND:Quercetin, a pigment (flavonoid) found in many plants and foods, has good effects on protecting liver function but poor solubility and bioavailability in vivo. A drug delivery system can improve the accumulation and bioavailability of quercetin in liver. In this study, we used liposomal nanoparticles to entrap quercetin and evaluated its protective and therapeutic effects on drug-induced liver injury in rats. METHODS: The nanoliposomal quercetin was prepared by a thin film evaporation-high pressure homogenization method and characterized by morphology, particle size and drug content. Acute liver injury was induced in rats by composite factors, including carbon tetrachloride injection, high-fat corn powder intake and ethanol drinking. After pure quercetin or nanoliposomal quercetin treatment, liver function was evaluated by detecting serum levels of glutamic-pyruvic transaminase (GPT), glutamic-oxal acetic transaminase (GOT) and direct bilirubin (DBIL). Histology of injured liver tissues was evaluated by hematoxylin and eosin staining. RESULTS: On histology, liposomal nanoparticles loading quercetin were evenly distributed spherical particles. The nanoliposomal quercetin showed high bioactivity and bioavailability in rat liver and markedly attenuated the liver index and pathologic changes in injured liver tissue. With nanoliposomal quercetin treatment, the serum levels of GPT, GOT and DBIL were significantly better than treated with pure quercetin. Using liposomal nanoparticles to entrap quercetin might be an effective strategy to reduce hepatic injury and protect hepatocytes against damage. CONCLUSION: Liposomal nanoparticles may improve the solubility and bioavailability of quercetin in liver. Furthermore, nanoliposomal quercetin could effectively protect rats against acute liver injury and may be a new hepatoprotective and therapeutic agent for patients with liver diseases.
Authors: Margarida Ferreira-Silva; Catarina Faria-Silva; Manuela C Carvalheiro; Sandra Simões; H Susana Marinho; Paulo Marcelino; Maria Celeste Campos; Josbert M Metselaar; Eduarda Fernandes; Pedro V Baptista; Alexandra R Fernandes; Maria Luísa Corvo Journal: Pharmaceutics Date: 2022-01-03 Impact factor: 6.321