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Glycyrrhetinic acid and TAT peptide modified dual-functional liposomes for treatment of hepatocellular cancer.

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资源类型：
Pubmed体系：
作者：
Huang Sixi[1] * ; Ren Di[1] ; Wu Xinrong[2] ; Li Ming[3] ; Yu Xuesong[3] ; Nie Xiaoling[1] ; Wang Ying[4,*2] ; Wang Yan[1,*1] ;
机构： [1]School of Traditional Chinese Medicine, Guangdong Pharmaceutical University, 510006 Guangzhou, China [2]GeneralHospital of Southern Theater Command, PLA, 510006 Guangzhou, China [3]School of Biosciences and Biopharmaceutics,Guangdong Pharmaceutical University, 510006 Guangzhou, China [4]School of Chemistry and Chemical Engineering,Guangdong Pharmaceutical University, 510006 Guangzhou, China
出处：
DOI： 10.2174/1568026620666200722110244
ISSN：

关键词： Liposomes 10-hydroxycamptothecin Glycyrrhetinic acid TAT peptide Hepatocellular cancer Tumor-targeting

摘要：
Surgery remains the front-line therapeutic strategy to treat early hepatocellular carcinoma (HCC), however the 5-year recurrence rates of HCC patients are high. 10-Hydroxycamptothecin (10-HCPT) is known anti-HCC agent but its poor solubility and bioavailability have limited its clinical use. In this study, we developed a novel nanoliposome encapsulated 10-hydroxycamptothecin modified with glycyrrhetinic acid (GA) and TAT peptide (GA/TAT-HCPT-LP) for the treatment of HCC. Dual modified GA and TAT can enhance tumor targeting and tumor penetration. The GA/TAT-HCPT-LP NPs were synthesized using the thin-film dispersion method. GA/TAT-HCPT-LP were characterized for particle size, zeta potential and morphology. Drug release from the GA/TAT-HCPT-LP liposomes was measured by dialysis. Cell-uptake was assessed by microscopy and flow cytometry. Cell proliferation, migration and apoptosis were measured to evaluate in vitro antitumor activity of GA/TAT-HCPT-LP via CCK-8 assays, Transwell assays, and flow cytometry, respectively. The in vivo distribution of GA/TAT-HCPT-LP was evaluated in HCC animal models. Tumor-bearing mouse models were used to assess the in vivo therapeutic efficacy of GA/TAT-HCPT-LP. The mean particle size and mean zeta potential of GA/TAT-HCPT-LP were 135.55 ± 2.76 nm and -4.57 ± 0.23 mV, respectively. Transmission electron micrographs (TEM) showed that the GA/TAT-HCPT-LP had a near spherical shape and a double-membrane structure. GA/TAT-HCPT-LP led to slow and continuous drug release, and could bind to HepG2 cells more readily than other groups. Compared to control groups, treatment with GA/TAT-HCPT-LP had a significantly large effect on inhibiting cell proliferation, tumor cell migration and cell apoptosis. In vivo assays showed that GA/TAT-HCPT-LP selectively accumulated in tumor tissue with obvious antitumor efficacy. In conclusion, the obtained GA/TAT-HCPT-LP could effectively target tumor cells and enhance cell penetration, highlighting its potential for hepatocellular cancer therapy. Copyright© Bentham Science Publishers; For any queries, please email at epub@benthamscience.net.

基金：
The current study was supported by the National Natural Science Foundation of China (No. 81673608), Guangdong Science and Technology Project(No. 2015A020211034; 2017A020215140), and Guangzhou Science and Technology Project (No.201707010155).
语种：
外文
PubmedID：
中科院(CAS)分区：
出版当年[2019]版：
大类 | 3 区 医学
小类 | 3 区 药物化学
最新[2025]版：
大类 | 4 区 医学
小类 | 4 区 药物化学
第一作者：
第一作者机构： [1]School of Traditional Chinese Medicine, Guangdong Pharmaceutical University, 510006 Guangzhou, China
通讯作者：
通讯机构： [1]School of Traditional Chinese Medicine, Guangdong Pharmaceutical University, 510006 Guangzhou, China [4]School of Chemistry and Chemical Engineering,Guangdong Pharmaceutical University, 510006 Guangzhou, China [*1]School of Traditional Chinese Medicine, Guangdong Pharmaceutical University, Guangzhou, 510006, China [*2]School of Chemistry and Chemical Engineering, Guangdong Pharmaceutical University, Guangzhou, 510006, China
推荐引用方式(GB/T 7714)：
Huang Sixi,Ren Di,Wu Xinrong,et al.Glycyrrhetinic acid and TAT peptide modified dual-functional liposomes for treatment of hepatocellular cancer.[J].Current topics in medicinal chemistry.2020,20(27):2493-2505.doi:10.2174/1568026620666200722110244.
APA：
Huang Sixi,Ren Di,Wu Xinrong,Li Ming,Yu Xuesong...&Wang Yan.(2020).Glycyrrhetinic acid and TAT peptide modified dual-functional liposomes for treatment of hepatocellular cancer..Current topics in medicinal chemistry,20,(27)
MLA：
Huang Sixi,et al."Glycyrrhetinic acid and TAT peptide modified dual-functional liposomes for treatment of hepatocellular cancer.".Current topics in medicinal chemistry 20..27(2020):2493-2505

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