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Legumain酶和线粒体双级靶向去氢骆驼蓬碱脂质体的制备及其体外特性评价
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| 篇名： | Legumain酶和线粒体双级靶向去氢骆驼蓬碱脂质体的制备及其体外特性评价 |
| TITLE： | Preparation of Legumain enzyme and mitochondrial double-stage targeted harmine liposome and evaluation of its in vitro characterization |
| 摘要： | 目的 制备Legumain酶和线粒体双级靶向去氢骆驼蓬碱（HM）脂质体（KA@HM-LPS），并对其制剂学特性、体外抗肿瘤作用及生物相容性进行初步评价。方法首先，筛选KA@HM-LPS的制备方法和均质化方法，并对制备的脂质体进行表征。其次，分别测定KA@HM-LPS的血清稳定性、体外释放率、溶血百分数，以及空白脂质体作用下的细胞存活率。最后，分别测定KA@HM-LPS作用下的细胞存活率、线粒体靶向性和对肝癌细胞迁移和侵袭的抑制作用。结果选择薄膜分散法制备KA@HM-LPS，其包封率为（90.50±0.62）％；选择挤出法作为KA@HM-LPS的均质化方法。所制备的KA@HM-LPS粒径、多分散系数、Zeta电位分别为（211.40±11.67）nm、0.316±0.014和（－14.20±0.49）mV。在37℃、10％胎牛血清中，12h后KA@HM-LPS的粒径基本稳定；KA@HM-LPS在20％血浆中的体外释放曲线符合Weibull分布，具有缓释效果；当HM质量浓度为160μg/mL时，KA@HM-LPS的溶血百分数为（4.23±0.19）％，远小于游离HM，具有安全性。当空白脂质体的质量浓度达400μg/mL时，LO2细胞的存活率为（94.40±6.12）％，载体生物相容性较好。体外细胞实验结果显示，KA@HM-LPS对Legumain酶过表达的肝癌细胞LGMN+-SK-Hep-1的抑制作用显著高于对正常肝癌细胞SK-Hep-1的抑制作用；且与SK-Hep-1细胞相比，LGMN+-SK-Hep-1细胞对载体的摄取效率更高；KA@HM-LPS可以更明显地抑制LGMN+-SK-Hep-1细胞的迁移和侵袭。结论成功制备KA@HM-LPS；该脂质体可以有效抑制Legumain酶过表达的肝癌细胞的迁移和侵袭，并提高HM的血液相容性。 |
| ABSTRACT： | OBJECTIVE To prep are Legumain enzyme and mitochondrial double-stage targeted harmine （HM） liposome （KA@HM-LPS）and preliminary evaluate its pharmaceutical properties ，in vitro antitumor effect and biocompatibility. METHODS Firstly，the preparation and homogenization methods of KA@HM-LPS was screened ，and prepared liposomes were characterized. Secondly，the serum stability ，in vitro release rate ，hemolysis percentage of KA@HM-LPS and cell survival rate under KA@BLPS were determines respectively. Finally ，the cell surivival rate ，mitochondrial targeting and inhibitory effects on cell migration and invasion of KA@HM-LPS were determined. RESULTS KA@HM-LPS was prepared by the thin-film dispersion method ，with encapsulation efficiency of （90.50 ± 0.62）％ . The extrusion moulding method was selected as homogenization method of KA@HM-LPS. The particle size ，polydispersity index ，and Zeta potential of KA@HM-LPS were （211.40±11.67）nm，0.316± 0.014 and（－14.20±0.49）mV，respectively. In 37 ℃，10％ FBS，the particle size of KA@HM-LPS kept stable after 12 h. In vitro release curve of KA@HM-LPS in 20％ plasma conformed to Weibull distribution and had the property of sustained release. When HM concentration was 160 μg/mL，the hemolysis percentage of KA@HM-LPS was （4.23±0.19）％，which was much lower than that of free HM ，with safety. When the mass concentration of KA@BLPS reaches 400 μg/mL，the survival rate of LO 2 cells was （94.40 ± 6.12）％ ，and the biocompatibility was good. Cell test results in vitro showed that ，inhibitory effect of KA@HM-LPS on liver cancer cells with overexpression of Legumain enzyme （LGMN -SK-Hep-1） was significantly higher than that of normal liver cancer cells SK-Hep- 1； compared with SK-Hep-1，LGMN +-SK-Hep-1 cells had a higher uptake efficiency of the liposome ；KA@HM-LPS could significantly inhibit the migration and invasion of LGMN +- SK-Hep-1 cells. CONCLUSIONS KA@HM-LPS is prepared successfully ，which can effectively inhibit the migration and invasion of liver cancer cells with Legumain enzyme overexpression ，and improve the blood compatibility of HM. |
| 期刊： | 2022年第33卷第13期 |
| 作者： | 伊帕尔古丽·阿皮孜，贺宏吉，王昭志，李喆喆，卡迪热娅·艾克拉木，白静雅，王梅 |
| AUTHORS： | Ipargul·Hafiz，HE Hongji ，WANG Zhaozhi ，LI Zhezhe ，Kadirya·Akram，BAI Jingya ，WANG Mei |
| 关键字： | 去氢骆驼蓬碱；线粒体；Legumain酶；脂质体 |
| KEYWORDS： | harmine；mitochondria；Legumain enzyme ；liposome |
| 阅读数： | 150 次 |
| 本月下载数： | 2 次 |
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