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羧化壳聚糖改善多肽蛋白类口服传递系统的研究

Study on improving the oral delivery system of peptide proteins by carboxylated chitosan

来源期刊: 广州医药 | 68-72 发布时间:2021-11-29 收稿时间:2025/11/13 17:20:31 阅读量:20
作者:
关键词:
壳聚糖纳米粒羧化壳聚糖口服蛋白类药物肠跨膜转运
DOI:
10.3969/j.issn.1000-8535.2018.04.018
收稿时间:
2017-12-15 
修订日期:
 
接收日期:
 
引用总数:
0  
目的 制备以牛血清白蛋白为模型药物的壳聚糖纳米制剂(BAS/CS NPs)及其体内外性质的研究,并通过加入羧化壳聚糖(WCS)来改善聚阳离子制备的纳米粒(CS NPs)的安全性。方法 利用油包水乳化-冻干法制备而得的CS NPs,通过激光粒度分析仪测定纳米粒粒径和电荷,用BCA法测定纳米粒包封率和载药量,并用Caco-2 cells单层膜模型评价BAS/CS NPs的细胞摄取情况和跨膜转运,以Franz扩散池法考察吸收考察BAS/CS NPs的离体各个小肠段黏膜的渗透性能,采用荧光分光光度计测定累积渗透量。结果 所制备的BAS/CS NPs平均粒径 在100~500 nm之间,电荷(-42.32±2.56)mV,包封率为88.37±6.82(%),载药量7.48±0.50(%),细胞毒性和细胞摄取实验表明羧化壳聚糖的BAS/CS NPs能降低细胞的毒性,并发现在十二指肠纳米粒具有促进BSA吸收作用(P<0.05)。结论 BAS/CS NPs是通过打开细胞紧密连接的方式增加BSA在小肠内的吸收。WCS降低BAS/CS NPs的细胞毒性,增强了兔小肠的BSA运输。作用要优于广泛研究的聚阳离子纳米粒体系,为口服蛋白类药物的传递提供了新的渠道。
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