双重响应靶向双药协同递送纳米系统的制备及体外评价
Chinese Journal of Hospital Pharmacy(2023)
Abstract
目的:制备双重响应靶向性双载药纳米粒(DOX/CMCS-ss-MTX NPs),并进行体外抗肿瘤考察.方法:甲氨蝶吟(MTX)通过二硫键接枝到羧甲基壳聚糖(CMCS)上,核磁共振氢谱(1 H-NMR)、红外光谱(IR)确证结构.离子交联法制备纳米粒,对粒径、Zeta电位进行表征;测定载阿霉素(DOX)和甲氨蝶吟(MTX)的DOX/CMCS-ss-MTX NPs包封率和载药量;MTT 实验考察 DOX/CMCS-ss-MTX NPs 体外抗肿瘤活性.结果:DOX/CMCS-ss-MTX NPs 粒径为(148.3±2.5)nm,阿霉素载药量为(17.10±0.28)%,包封率为(71.32±3.54)%;甲氨蝶吟载药量为(19.35±0.33)%,包封率为(86.9±2.35)%.实验证明其具有pH和还原响应,肿瘤微环境下可快速释放.MTT实验表明DOX/CMCS-ss-MTX NPs对正常肝细胞没有明显影响,对肝癌细胞有明显抑制作用.结论:DOX/CMCS-ss-MTX NPs粒径均一、载药量较高,具有良好的pH响应性和还原响应性,共同递送甲氨蝶呤和阿霉素,具有协同抗肿瘤效果.
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Key words
dual responsive,co-delivery,targeting,disulfide bond
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