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藤黄酸智能响应脂质体-水凝胶纳米制剂的制备、表征及体外抗肿瘤活性研究
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| 篇名： | 藤黄酸智能响应脂质体-水凝胶纳米制剂的制备、表征及体外抗肿瘤活性研究 |
| TITLE： | Preparation，characterization，and in vitro antitumor activity of Gambogic acid-loaded intelligent responsive liposome-hydrogel nanopreparation |
| 摘要： | 目的 制备藤黄酸（GA）智能响应脂质体-水凝胶纳米制剂，并对其进行表征和体外抗肿瘤活性研究。方法采用乙醇注入法结合冷溶法，将GA和光敏剂吲哚菁绿（ICG）联合制成智能响应脂质体-水凝胶纳米制剂（GA-ICG-Lip-gel）。观察GA-ICG-Lip-gel的外观形态和微观形态，测定其包封率和载药量，考察其光热转换性能、光热稳定性、红外成像性质，测定其体外释放度。以人源乳腺癌MCF-7细胞为研究对象，考察GA-ICG-Lip-gel（或结合近红外光照射）对细胞活力、迁移能力的影响以及细胞对GA-ICG-Lip-gel的摄取能力。结果GA-ICG-Lip-gel在室温下呈溶液状态，而在37℃下则为凝胶状态；其微观结构致密、孔隙较小，包封率为（96.07±0.86）%、载药量为（6.28±1.16）%；经近红外光照射后，GA-ICG-Lip-gel温度升至42℃以上，且升温曲线未出现明显衰减，升温效率同时依赖于照射时间与药物浓度；相比于不含明胶酶的介质，GA-ICG-Lip-gel在含明胶酶的介质中的累积释放率增加。体外实验结果显示，MCF-7细胞对GA-ICG-Lip-gel的摄取较强；GA-ICG-Lip-gel可显著抑制MCF-7细胞的活力和迁移能力（P＜0.05），且该抑制作用在近红外光照射下更强。结论本研究成功制备GA-ICG-Lip-gel，该制剂具有良好的光热转换性能和温度/酶双重响应性释药特征，且对乳腺癌细胞的增殖、迁移具有显著的抑制作用。 |
| ABSTRACT： | OBJECTIVE To prepare an intelligent responsive liposome-hydrogel nanopreparation co-loaded with gambogic acid （GA）， and characterize its antitumor activity in vitro . METHODS GA-ICG-Lip-gel was prepared by ethanol injection and cold dissolution， incorporating GA and the photosensitizer indocyanine green （ICG）. The appearance and microscopic morphology of GA-ICG-Lip-gel were observed， its encapsulation efficiency and drug loading capacity were measured， and its photothermal conversion performance， photothermal stability， and infrared imaging properties were investigated， along with the determination of its in vitro release profile. Human breast cancer MCF-7 cells were used as objects to investigate the effects of GA-ICG-Lip-gel （or with near-infrared light irradiation） on cell viability， migration ability， and the cellular uptake capacity of GA-ICG-Lip-gel. RESULTS GA-ICG-Lip-gel existed in a solution state at room temperature and transformed into a gel state at 37 ℃. Its microstructure was dense with small pores， and its encapsulation efficiency and drug loading were （96.07±0.86） % and （6.28±1.16） %， respectively. After exposure to near-infrared light， the temperature of GA-ICG-Lip-gel rose above 42 ℃， with no significant attenuation observed in the heating curve. The heating efficiency was dependent on both the irradiation time and drug concentration. Compared to media without gelatinase， the cumulative release rate of GA-ICG-Lip-gel increased in media containing gelatinase. In vitro studies showed that GA-ICG-Lip-gel could be efficiently taken up by MCF-7 cells； GA-ICG-Lip-gel significantly inhibited the viability and migration ability of MCF-7 cells （ P ＜0.05）， and this inhibitory effect was further enhanced under near-infrared light irradiation. CONCLUSIONS This study successfully prepares GA-ICG-Lip-gel， which exhibits favorable photothermal conversion properties and temperature/enzyme dual-responsive drug release characteristics， and demonstrates significant inhibitory effects on the proliferation and migration of breast cancer cells. |
| 期刊： | 2026年第37卷第05期 |
| 作者： | 陈宇；黄胜楠；王子昂；赵云龙；魏杲健；武思楠；关延彬；祝侠丽 |
| AUTHORS： | CHEN Yu，HUANG Shengnan，WANG Ziang，ZHAO Yunlong，WEI Gaojian，WU Sinan，GUAN Yanbin，ZHU Xiali |
| 关键字： | 藤黄酸；光敏剂；乳腺癌；脂质体水凝胶；光热治疗 |
| KEYWORDS： | gambogic acid； photosensitizer； breast cancer； liposome-hydrogel； photothermal therapy |
| 阅读数： | 1 次 |
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