| 冬凌草甲素聚乙二醇功能化氧化石墨烯纳米粒的制备及抗结肠癌实验研究 |
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| 引用本文： | 俞文英,马建琦,方杰,方晴霞,王露晨,莫丽,余陈欢. 冬凌草甲素聚乙二醇功能化氧化石墨烯纳米粒的制备及抗结肠癌实验研究[J]. 中草药, 2017, 48(19): 3954-3960 |
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| 作者姓名： | 俞文英 马建琦 方杰 方晴霞 王露晨 莫丽 余陈欢 |
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| 作者单位： | 浙江省医学科学院, 浙江 杭州 310013,浙江省医学科学院, 浙江 杭州 310013;杭州江干区人民医院, 浙江 杭州 310016,浙江省医学科学院, 浙江 杭州 310013,浙江中医药大学, 浙江 杭州 310053,浙江省医学科学院, 浙江 杭州 310013;浙江中医药大学, 浙江 杭州 310053,浙江省医学科学院, 浙江 杭州 310013;浙江中医药大学, 浙江 杭州 310053,浙江省医学科学院, 浙江 杭州 310013 |
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| 基金项目： | 浙江省科技厅院所专项（2015F50065，2014F10033） |
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| 摘 要： | 目的制备负载冬凌草甲素(oridonin,ORI)的聚乙二醇功能化氧化石墨烯(PEGylated graphene oxide,GO-PEG)纳米粒(nanoparticles,NPs),并探讨其对结肠癌的抑制作用。方法利用酰胺化反应将端基为氨基的四臂聚乙二醇(PEG)连到氧化石墨烯(GO)上,并通过红外光谱(IR)和差示-热重联用热分析仪(TGA)等对其进行表征;再通过物理共混的方法在GO-PEG上负载抗肿瘤药物ORI,紫外光谱(UV)法测其包封率和载药率,MTT法测定载药体系对人结肠癌细胞SW620和HT29的增殖毒性,并建立荷瘤裸鼠模型考察其体内抗肿瘤活性。结果 IR和TGA测定结果表明PEG已成功偶联到GO上,UV法测得ORI-GO-PEG的包封率和载药率分别为95.81%和48.92%,且在各种生理溶液中具有良好的稳定性。体外细胞毒性实验结果表明,与ORI裸药相比,ORI-GO-PEG-NPs对结肠癌细胞的杀伤能力更强。体内抑瘤实验进一步发现,ORI-GO-PEG-NPs可以更好地抑制体内SW620肿瘤的生长。结论制得的ORI-GO-PEG-NPs具有优良的载药性能和较强的抗结肠癌作用,为今后开发抗肿瘤药物纳米给药系统提供了实验依据。
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| 关 键 词： | 氧化石墨烯 冬凌草甲素 聚乙二醇 纳米粒 药物传输 结肠癌 红外光谱 差示-热重联用热分析 包封率 载药率 增殖 抗肿瘤活性 |
| 收稿时间： | 2017-04-24 |
Preparation of PEGylated graphene oxide nanoparticles loaded with oridonin and its inhibitory effects on human colon cancer |
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| YU Wen-ying,MA Jian-qi,FANG Jie,FANG Qing-xi,WANG Lu-chen,MO Li and YU Chen-huan. Preparation of PEGylated graphene oxide nanoparticles loaded with oridonin and its inhibitory effects on human colon cancer[J]. Chinese Traditional and Herbal Drugs, 2017, 48(19): 3954-3960 |
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| Authors: | YU Wen-ying MA Jian-qi FANG Jie FANG Qing-xi WANG Lu-chen MO Li YU Chen-huan |
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| Affiliation: | Zhejiang Academy of Medical Sciences, Hangzhou 310013, China,Zhejiang Academy of Medical Sciences, Hangzhou 310013, China;Hangzhou Jianggan District People''s Hospital, Hangzhou 310016, China,Zhejiang Academy of Medical Sciences, Hangzhou 310013, China,Zhejiang Chinese Medical University, Hangzhou 310053, China,Zhejiang Academy of Medical Sciences, Hangzhou 310013, China;Zhejiang Chinese Medical University, Hangzhou 310053, China,Zhejiang Academy of Medical Sciences, Hangzhou 310013, China;Zhejiang Chinese Medical University, Hangzhou 310053, China and Zhejiang Academy of Medical Sciences, Hangzhou 310013, China |
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| Abstract: | Objective To prepare PEGylated graphene oxide nanoparticles (GO-PEG-NPs) loaded with oridonin (ORI) and investigate its inhibitory effect on human colon cancer. Methods 4-armed PEG was grafted onto GO via an amidation process and GO-PEG was characterized by IR and TGA. Then, ORI, a widely used cancer chemotherapy drug, was absorbed onto GO-PEG via blending. The encapsulation efficiency and drug loading ratio were measured by UV. The cytotoxicity of ORI-GO-PEG, GO-PEG, and free ORI on SW620 and HT29 human colon cancer cells were evaluated using MTT assay. In vivo anti-tumor activity of ORI-GO-PEG-NPs were evaluated in mice bearing SW620 tumor. Results IR and TGA data indicated that 4-armed PEG was successfully coupled with GO and UV data showed that the encapsulation efficiency and drug loading ratio were 95.81% and 48.92%, respectively. Moreover, ORI-GO-PEG-NPs showed good stability in physiological condition. The results of cytotoxicity test indicated that compared to free ORI, the ORI-GO-PEG-NPs exhibited higher cytotoxicity in SW620 and HT29 cells. Meanwhile, it was confirmed that ORI-GO-PEG-NPs could significantly inhibit the growth of SW620 tumor in vivo compared with ORI. Conclusion The obtained ORI-GO-PEG-NPs displayed excellent drug-loading capacity and better tumor inhibitory effect. These results provided the experimental basis for development of anticancer drug delivery system. |
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| Keywords: | graphene oxide oridonin polyethylene glycol nanoparticles drug delivery colon cancer infrared spectrometry differential scanning calorimetry-thermogravimetry analysis encapsulation efficiency loading efficiency cell proliferation anti-tumor activity |
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