Abstract
Background: Liver cancer is a common malignant tumor worldwide, and its morbidity and mortality increase each year. The disease has a short course and high mortality, making it a serious threat to human health. Purpose: The objective of this study was to create novel liver-targeting nanoliposomes to encapsulate cantharidin (CTD) as a potential treatment for hepatic carcinoma. Methods: 3-Galactosidase-30-stearyl deoxyglycyrrhetinic acid (11-DGA-3-O-Gal)-modified liposomes (11-DGA-3-O-Gal-CTD-lip) for the liver-targeted delivery of CTD were prepared via the film-dispersion method and characterized. In vitro analyses of the effects on cellular cytotoxicity, cell migration, cell cycle, and cell apoptosis were carried out and an in vivo pharmacokinetics study and tissue distribution analysis were performed. Results: Compared with unmodified liposomes (CTD-lip), 11-DGA-3-O-Gal-CTD-lip showed higher cytotoxicity and increased the inhibition of HepG2 cell migration, but they did not increase the apoptotic rate of cells. The inhibition mechanism of 11-DGA-3-O-Gal-CTD-lip on hepatocellular carcinoma was partly through cell cycle arrest at the S phase. Analysis of pharmacokinetic parameters indicated that 11-DGA-3-O-Gal-CTD-lip were eliminated more rapidly than CTD-lip. Regarding tissue distribution, the targeting efficiency of 11-DGA-3-O-Gal-CTD-lip to the liver was (41.15 ± 3.28)%, relative targeting efficiency was (1.53 ± 0.31)%, relative uptake rate was( 1.69 ± 0.37)%, and peak concentration ratio was (2.68 ± 0.12)%. Conclusion: 11-DGA-3-O-Gal-CTD-lip represent a promising nanocarrier for the liver-targeted delivery of antitumor drugs to treat hepatocellular carcinoma.
Highlights
As a major public health concern worldwide, cancer has received widespread attention from all parts of society, but the burden of cancer will increase in coming decades, especially in low- and middle-income countries (LMIC) [1,2]
The 13 C-nuclear magnetic resonance (NMR) spectrum of 3-acetylation-galactosidase-30-stearyl deoxyglycyrrhetinic acid showed that the chemical shift values at the C3 atom was shifted to a lower magnetic field (δ79.03→δ90.92), which indicated esterification proceeded between DGA and acetobromo-α-d-galactose
The purified DGA, 3-acetylation-galactosidase-30-stearyl deoxyglycyrrhetinic acid and 11-DGA-3-O-Gal were analyzed by mass spectrometry (MS) and NMR spectroscopy
Summary
As a major public health concern worldwide, cancer has received widespread attention from all parts of society, but the burden of cancer will increase in coming decades, especially in low- and middle-income countries (LMIC) [1,2]. Primary liver cancer, comprised majorly of hepatocellular carcinoma (HCC) and intrahepatic cholangiocarcinoma, had become the 5th most common malignant tumor, the 2th cause of cancer death worldwide in 2018 [4]. HCC is one of the most common malignant tumors worldwide, and its morbidity and mortality increase each year [5,6]. HCC has a short course of disease and high mortality, presenting a serious threat to human health. Liver cancer is a common malignant tumor worldwide, and its morbidity and mortality increase each year. Purpose: The objective of this study was to create novel liver-targeting nanoliposomes to encapsulate cantharidin (CTD) as a potential treatment for hepatic carcinoma. The inhibition mechanism of 11-DGA-3-O-Gal-CTD-lip on hepatocellular carcinoma was partly through cell cycle arrest at the S phase.
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