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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 ·
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