习彦茹,崔铭姝,王熙宇,朱澄云,徐璐
XI Yanru,CUI Mingshu,WANG Xiyu,ZHU Chengyun,XU Lu

• 1:沈阳药科大学药学院
• 2:沈阳药科大学制药工程学院

摘要(Abstract)：

目的 在构建沸石咪唑酯骨架材料(zeolitic imidazolate framework, ZIF)-90纳米载体的基础上，修饰叶酸(folic acid, FA),并对其作为药物载体的可行性进行了初步评价。方法 制备ZIF-90-FA纳米载体，通过透射电子显微镜、比表面及孔径分析仪和动态光散射仪对纳米载体进行表征；以盐酸阿霉素(doxorubicin hydrochloride, DOX)为模型药物构建DOX@ZIF-90-FA纳米药物递送系统，对其体外释放行为进行考察；通过溶血实验和细胞毒性实验初步评价载体的生物学性质；通过药效学研究对载药系统的体外抗肿瘤效果进行初步探究。结果 ZIF-90-FA具有较高的药物负载能力(22.72%),构建的DOX@ZIF-90-FA载药体系具有pH敏感性释放行为，在磷酸盐缓冲液(pH 5.0)中累积释放量为65.57%,在磷酸盐缓冲液(pH 7.4)中累积释放量为21.50%。ZIF-90-FA纳米载体的溶血率和细胞毒性均较低，且DOX@ZIF-90-FA具有较好的体外抗肿瘤活性。结论 ZIF-90-FA纳米载体的高负载能力、低毒性及良好的生物相容性使其有望作为药物载体应用于生物医学领域。
Objective Folic acid modified zeolitic imidazolate framework-90(ZIF-90-FA) nanoparticles were synthesized by zeolitic imidazolate framework-90(ZIF-90) and folic acid(FA), and ZIF-90-FA as drug carriers were used to evaluated the feasibility.Methods ZIF-90-FA nanoparticles were characterized by transmission electron microscopy(TEM),Brunauer-Emmett-Teller(BET),and dynamic laser light scattering(DLS);Then, doxorubicin hydrochloride(DOX),as a model drug, was loaded in ZIF-90-FA nanoparticles to construct a DOX@ZIF-90-FA nano drug delivery system, then the drug release behavior in vitro was investigated; Moreover, hemolysis test and cytotoxicity test were carried out to evaluate the biological properties of ZIF-90-FA nano carriers; Finally, the anti-tumor effect of drug delivery system in vitro was preliminarily explored through cytotoxicity test.Results ZIF-90-FA nano carriers were with high drug loading capacity of 22.72%.And the constructed drug delivery system manifested a pH-sensitive drug release behavior, which the cumulative release amount was 65.57% in PBS 5.0,but only 21.50% in PBS 7.4.ZIF-90-FA nano carriers showed low hemolysis ratio and cytotoxicity.DOX@ZIF-90-FA drug delivery system exhibited a good anti-tumor activity in vitro.Conclusion The high loading capacity, low toxicity and good biocompatibility of ZIF-90-FA nanoparticles make them feasible to be used as drug carriers in biomedical field.

关键词(KeyWords)： ZIF-90-FA;纳米载体;pH敏感;盐酸阿霉素
ZIF-90-FA;nano carrier;pH-sensitive;doxorubicin hydrochloride

Abstract:

Keywords:

基金项目(Foundation):

作者(Author): 习彦茹,崔铭姝,王熙宇,朱澄云,徐璐
XI Yanru,CUI Mingshu,WANG Xiyu,ZHU Chengyun,XU Lu

DOI: 10.14066/j.cnki.cn21-1349/r.2021.0649

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