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学报
               206                 Journal of China Pharmaceutical University 2026, 57(2): 206 − 214


                 胰腺癌靶向纳米载体的合成、表征及其改善光动力治疗研究



                                                   乔佳男     1,2,3* ,田烽椿   3


                 ( 南京中医药大学附属中西医结合医院, 南京             210028; 江苏省中医药研究院, 中药组分与微生态研究中心, 南京              210028;
                                                          2
                  1
                                                 中国药科大学药学院, 南京 211198)
                                                3
               摘 要 采用点击化学方法合成了一种胰腺癌靶向纳米载体                     LL-PTP,物理包载难溶性光敏药物酞菁锌(ZnPc)制备成               LL-
               PTP/ZnPc 纳米粒。LL-PTP   临界聚集浓度为       52.97 μg/mL,物理包载  ZnPc 形成的  LL-PTP/ZnPc 纳米粒为蓝色透明溶液,
               ZnPc 载药量为(20.1±1.4)%,水合粒径为(89.18±0.21)nm,具有良好的放置稳定性和血清稳定性,符合临床对注射剂型稳
               定性的要求,并且      LL-PTP/ZnPc 在肿瘤组织中释药比例可达到血清中的             6 倍以上,有利于纳米粒在肿瘤组织中发挥治疗作
               用。分别经激光共聚焦显微镜和流式细胞术进行定性和定量研究                        LL-PTP/ZnPc 靶向摄取行为,结果表明,LL-PTP/ZnPc 通
               过  Plectin-1 介导的胞吞作用增加    PANC-1 细胞对纳米粒摄取,效率显著优于           LL/ZnPc 和游离  ZnPc。探针  DCFH-DA  检测胞
               内  ROS  水平结果显示,光照     LL-PTP/ZnPc 诱导胞内  ROS  生成,有利于在胰腺癌中发挥更好的光动力治疗作用。综上,本研
               究成功制备了胰腺癌靶向纳米载体            LL-PTP,并成功负载    ZnPc,改善其光动力治疗效果。
               关键词 胰腺癌;靶向纳米载体;光动力治疗;纳米载体合成;纳米载体表征;光动力治疗增效
               中图分类号  R944       文献标志码 A             文章编号 1000−5048(2026)02−0206−09
                                                     doi:10.11665/j.issn.1000−5048.2025090601

                引用本文 乔佳男,田烽椿. 胰腺癌靶向纳米载体的合成、表征及其改善光动力治疗研究                  [J]. 中国药科大学学报,2026,57(2):206-214.

                Cite  this  article  as:  QIAO  Jianan,  TIAN  Fengchun.  Synthesis,  characterization  and  application  of  targeted  nanocarrier  improving
                photodynamic therapy for pancreatic cancer[J]. J China Pharm Univ, 2026, 57(2): 206-214.


               Synthesis, characterization and application of targeted nanocarrier improving
               photodynamic therapy for pancreatic cancer
               QIAO Jianan 1,2,3* , TIAN Fengchun 3
               1
                Affiliated  Hospital  of  Integrated  Traditional  Chinese  and  Western  Medicine,  Nanjing  University  of  Chinese  Medicine,  Nanjing
                      2
               210028;  Research  Center  for  Microecology  of  Functional  Components  in  Traditional  Chinese  Medicines,  Jiangsu  Provincial
                                                  3
               Academy of Chinese Medicine, Nanjing 210028;  School of Pharmacy, China Pharmaceutical University, Nanjing 211198, China

               Abstract    LL-PTP,  a  pancreatic  cancer-targeted  nanocarrier,  was  synthesized  via  click  chemistry,  and  the
               insoluble  photosensitive  drug  zinc  phthalocyanine  (ZnPc)  was  physically  encapsulated  within  LL-PTP  to
               fabricate LL-PTP/ZnPc nanoparticles. The critical aggregation concentration (CAC) of LL-PTP was determined
               to be 52.97 μg/mL; the LL-PTP/ZnPc nanoparticles, formed by the physical encapsulation of ZnPc, appeared as a
               blue transparent solution; the ZnPc loading efficiency of these nanoparticles was (20.1 ± 1.4) %, with a hydrated
               particle  size  of  (89.18  ±  0.21)  nm;  notably,  the  nanoparticles  exhibited  excellent  storage  stability  and  serum
               stability,  which  fully  meet  the  stability  requirements  for  injectable  formulations  in  clinical  applications;
               furthermore,  the  release  rate  of  LL-PTP/ZnPc  in  tumor  tissue  was  significantly  higher  (6.2-fold)  than  that  in
               serum, which is significantly beneficial for the therapeutic effect of nanoparticles at the tumor site. To investigate
               the targeted uptake of LL-PTP/ZnPc, qualitative and quantitative analyses were performed using confocal laser
               scanning microscopy (CLSM) and flow cytometry, respectively, with the result that LL-PTP/ZnPc enhanced the
               uptake of nanoparticles by PANC-1 cells (a pancreatic cancer cell line) through Plectin-1-mediated endocytosis


                    收稿日期 2025-09-06  * 通信作者    E-mail:764579493@qq.com
                    基金项目    国家自然科学基金项目(No. 82404550);江苏省自然科学基金项目(BK20221044)
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