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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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陈 宇 ,黄胜楠 ,王子昂 ,赵云龙 ,魏杲健 ,武思楠 ,关延彬 ,祝侠丽 (1. 河南中医药大学药学院,郑州
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450046;2.河南中医药大学中医药科学院,郑州 450046)
中图分类号 R943 文献标志码 A 文章编号 1001-0408(2026)05-0613-07
DOI 10.6039/j.issn.1001-0408.2026.05.11
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。
关键词 藤黄酸;光敏剂;乳腺癌;脂质体水凝胶;光热治疗
Preparation, characterization, and in vitro antitumor activity of Gambogic acid-loaded intelligent
responsive liposome-hydrogel nanopreparation
CHEN Yu ,HUANG Shengnan ,WANG Ziang ,ZHAO Yunlong ,WEI Gaojian ,WU Sinan ,GUAN Yanbin ,
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ZHU Xiali (1. Pharmacy College, Henan University of Chinese Medicine, Zhengzhou 450046, China;2.
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Academy of Chinese Medical Science, Henan University of Chinese Medicine, Zhengzhou 450046, China)
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
Δ 基金项目 国家自然科学基金面上项目(No.82574878);河南省
高等学校重点科研项目(No.23A360007);河南省科技攻关项目 (P<0.05), and this inhibitory effect was further enhanced
(No.262102311256) under near-infrared light irradiation. CONCLUSIONS This
*第一作者 硕士研究生。研究方向:中药新剂型、新技术与评价。
study successfully prepares GA-ICG-Lip-gel, which exhibits
E-mail:yunchenshi@163.com
favorable photothermal conversion properties and temperature/
# 通信作者 教授,博士生导师。研究方向:中药新剂型、新技术与
评价。E-mail:zhuxiali1980@126.com enzyme dual-responsive drug release characteristics, and
中国药房 2026年第37卷第5期 China Pharmacy 2026 Vol. 37 No. 5 · 613 ·

