pH响应双载药抗肿瘤药物胶束的制备及性能研究
PDF下载 (7728)牛立敬,李博文,邱乾坤,冉 佳,赵玲玲 *,梁洪泽.pH响应双载药抗肿瘤药物胶束的制备及性能研究[J].宁波大学学报(理工版),2018,31(5):96-101.DOI:
NIU Li-jing,LI Bo-wen,QIU Qian-kun,RAN Jia,ZHAO Ling-ling *,LIANG Hong-ze.pH-triggered doxorubicin and paclitaxel co-delivery micellar system for anticancer drug delivery[J].Journal of Ningbo University(Natural Science & Engineering Edition),2018,31(5):96-101.DOI:
| Title: | pH-triggered doxorubicin and paclitaxel co-delivery micellar system for anticancer drug delivery |
| 作者: | 牛立敬, 李博文, 邱乾坤, 冉 佳, 赵玲玲 *, 梁洪泽 |
| Author(s): | NIU Li-jing, LI Bo-wen, QIU Qian-kun, RAN Jia, ZHAO Ling-ling *, LIANG Hong-ze |
| 关键词: | 阿霉素; 紫杉醇; 胶束; pH敏感; 药物释放 |
| Keywords: | DOX; PTX; micelles; pH-sensitive; drug release |
| 分类号: | TQ937 |
| 文献标识码: | A |
| 摘要: | 针对肿瘤组织低pH值的生理微环境特点, 设计并制备了pH响应的双载药胶束. 将药物分子阿霉素与氧化葡聚糖通过pH敏感的亚胺键相结合, 合成阿霉素-氧化葡聚糖前药分子. 该前药分子在水溶液中能够自组装形成胶束, 可包封其他疏水性药物如紫杉醇, 实现多种药物的协同治疗. 用红外光谱、透射电镜和动态光散射等对该双载药胶束进行了表征, 并模拟人体生理环境进行了药物体外释放行为的研究. 结果表明, 阿霉素和紫杉醇在载药胶束内均能够持续释放, 且降低环境pH值均能加快药物释放的速度. 由于肿瘤组织的pH值比正常组织要低, 该双载药胶束的这种低pH值触发式药物释放行为对于肿瘤的治疗具有积极意义. |
| Abstract: | pH-sensitive and dual-drug loaded micelles for anticancer drug delivery are prepared based on aldehyde dextran according to the special physiological microenvironment of tumor tissue. Oxdex-DOX conjugates are firstly synthesized by conjugating DOX with the polymer chain of oxide dextran through pH-sensitive imine bond. The prodrug conjugates can assemble and form micelles in water, and hydrophobic drugs such as paclitaxel (PTX) can be loaded in the core of micelles to form dual-drug loaded micelles for the synergistic treatment of cancer. FTIR, and 1H NMR and dynamic light scattering are used to characterize the structure and property of the micelles. In vitro drug release shows that both DOX and PTX may release from the dual-drug loaded micelles for several days, and release rate of both drugs may be accelerated by lowering the media pH from 7.4 to 6.5 and 5.0. Due to the lower pH value of tumor tissue than normal tissue, the pH triggered drug release from the micelles is more conducive for cancer treatment. |
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| 备注/Memo: | 收稿日期: 2018－01－06. 宁波大学学报（理工版）网址: http://journallg.nbu.edu.cn/ 基金项目: 国家自然科学基金（51403108）; 宁波市自然科学基金（2016A610049）; 宁波大学王宽诚幸福基金. 第一作者: 牛立敬（1989－）, 女, 山东聊城人, 在读硕士研究生, 主要研究方向: 生物医用材料. E-mail: 862991390@qq.com *通信作者: 赵玲玲（1986－）, 女, 湖南会同人, 副教授, 主要研究方向: 生物医用材料. E-mail: zhaolingling@nbu.edu.cn 宁波大学学报（理工版）网址：http://journallg.nbu.edu.cn/ |
