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    Home > Active Ingredient News > Digestive System Information > Int J Pharm: Paeoniflorin-phospholipid complex micelles improve cholestatic liver injury

    Int J Pharm: Paeoniflorin-phospholipid complex micelles improve cholestatic liver injury

    • Last Update: 2022-02-16
    • Source: Internet
    • Author: User
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    Background: Cholestatic liver diseases , including primary cholangitis, primary sclerosing cholangitis, and estrogen-induced cholestasis, may progress to liver fibrosis, cirrhosis, and even liver cancer if treatment is delayed


    Cholestatic liver disease Cholestatic liver disease TLR4/MyD88/NF-κB TLR4/MyD88/NF-κB PXR/CAR PXR/CAR

    Paeoniflorin (PF) , a monoterpene glycoside compound, is beneficial in improving nonalcoholic fatty liver disease, liver I/R injury, arthritis and cholestatic liver disease, but its low bioavailability greatly limits clinical application


    Paeoniflorin (PF) Paeoniflorin (PF) Phospholipid (PL) Phospholipid (PL) Phospholipid Complex (PLC) Phospholipid Complex (PLC)

    OBJECTIVE: On the basis of previous studies, PF-PLC micelles were first prepared to study their protective effect on 17α-ethinyl estradiol (EE)-induced cholestatic liver injury in rats, and finally from inflammation and nuclear receptor/metabolism.


    Inflammation Inflammation Nuclear Receptor/Metabolic Enzyme Nuclear Receptor/Metabolic Enzyme

    Methods: PF-PLC micelles were prepared and characterized


    Liver Histopathology Liver Histopathology Inflammatory Cytokines Inflammatory Cytokines Inflammation-related Pathway Proteins Immunofluorescence Staining Immunofluorescence Staining Immunohistochemistry Immunohistochemistry

    Results: Compared with PF-PLC, PF-PLC micelles had better sustained release effect


    Serum levels of total bilirubin (TBIL), direct bilirubin (DBIL), and total bile acids (TBA) in EE-induced cholestasis rats were higher than those in controls, and PF and PF-PLC micelle treatment reduced these indicators


    Mechanistic studies showed that PF-PLC micelle treatment could inhibit the TLR4/MyD88/NF-κB pathway and further reduce the level of pro-inflammatory factors


    Conclusion: These results indicate that PF-PLC micelles have great potential in the treatment of cholestatic liver disease, and provide a scientific experimental basis for the clinical development of a novel PF hepatoprotective drug delivery system


    PF-PLC micelles have great potential in the treatment of cholestatic liver disease

    Source:

    Yuan, T.


    Yuan, T.
    , Lv, S.
    , Zhang, W.
    , et al.
    (2022).
    PF-PLC micelles ameliorate cholestatic liver injury via regulating TLR4/MyD88/NF-κB and PXR/CAR/UGT1A1 signaling pathways in EE- induced rats.
    International journal of pharmaceutics, 615, 121480.
    Advance online publication.
    https://doi.
    org/10.
    1016/j.
    ijpharm.
    2022.
    121480

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