ReferenceID 4583
Liver-targeted delivery of asiatic acid nanostructured lipid carrier for the treatment of liver fibrosis
Drug Deliv
Liver fibrosis is a major global health concern. Management of chronic liver disease is severely restricted in clinics due to ineffective treatment approaches. However, a lack of targeted therapy may aggravate this condi
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Record Fields
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- Reference Id
- 4583
- Evidence Id
- 21173
- Core Evidence Id
- 21173
- Source Reference Id
- 2436
- Herb2 Reference Id
- HBREF003233
- Subject Paper Key
- HBIN017057_34854788
- Pubmed Id
- 34854788
- Doi
- 10.1080/10717544.2021.2008054
- Paper Title
- Liver-targeted delivery of asiatic acid nanostructured lipid carrier for the treatment of liver fibrosis
- Paper Abstract
- Liver fibrosis is a major global health concern. Management of chronic liver disease is severely restricted in clinics due to ineffective treatment approaches. However, a lack of targeted therapy may aggravate this condition. Asiatic acid (AA), a pentacyclic triterpenoid acid, can effectively protect the liver from hepatic disorders. However, the pharmaceutical application of AA is limited by low oral bioavailability and poor targeting efficiency. This study synthesized a novel liver-targeting material from PEG-SA, chemically linked to ursodeoxycholic acid (UA), and utilized it to modify AA nanostructured lipid carriers (UP-AA-NLC) with enhanced targeting and improved efficacy. The formulation of UP-AA-NLC was optimized via the Box-Behnken Experimental Design (BBD) and characterized by size, zeta potential, TEM, DSC, and XRD. Furthermore, in vitro antifibrotic activity and proliferation of AA and NLCs were assessed in LX-2 cells. The addition of UP-AA-NLC significantly stimulated the TGF-beta1-induced expression of alpha-SMA, FN1, and Col I alpha1. In vivo near-infrared fluorescence imaging and distribution trials in rats demonstrated that UP-AA-NLC could significantly improve oral absorption and liver-targeting efficiency. Oral UP-AA-NLC greatly alleviated carbon tetrachloride-induced liver injury and fibrosis in rats in a dosage-dependent manner, as reflected by serum biochemical parameters (AST, ALT, and ALB), histopathological features (H&E and Masson staining), and antioxidant activity parameters (SOD and MDA). Also, treatment with UP-AA-NLC lowered liver hydroxyproline levels, demonstrating a reduction of collagen accumulation in the fibrotic liver. Collectively, optimized UP-AA-NLC has potential application prospects in liver-targeted therapy and holds great promise as a drug delivery system for treating liver diseases.
- Journal
- Drug Deliv
- Publish Year
- 2021
- Experiment Subject
- rat; lx-2 cells
- Experiment Type
- Cell Experiment
- Phenotype Related
- Liver Fibrosis; Hepatic Disorders; Chronic Liver Disease; Liver Diseases; Fibrosis
- Paper Title Cn
- Paper Title En
- Liver-targeted delivery of asiatic acid nanostructured lipid carrier for the treatment of liver fibrosis
- Bilingual Status
- semi_complete