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制备含有amintoflavone的DSPE-PEG₂₀₀₀小粒,提高了生物可用性和体外抗瘤功效

Yuan Feng¹, Jin Wang¹, Shuaishuai Zhang²

¹Hebei Key Laboratory of Neuropharmacology, Hebei North University, Zhangjiakou, China.

Biomedical chromatography : BMC

|June 20, 2023

概括

聚乙烯甘) - 迪斯泰洛酸乙醇胺 (DSPE-PEG) 微粒显著改善了阿门托弗拉 (AF) 溶解度和口服生物可用性. 这些新型菌根增强了AF.

科学领域:

纳米技术纳米技术
材料科学材料科学材料科学
药理学药理学是指药理学的学科.

背景情况:

阿门托弗拉 (AF) 显示出有前途的抗癌性质,但其水溶性较差,限制了其治疗应用.
开发有效的药物输送系统对于提高AF等难溶化合物的生物可用性和有效性至关重要.

研究的目的:

使用聚乙烯糖醇-二二酸乙醇胺 (DSPE-PEG) 制备含有amintoflavone (AF) 的小粒,以提高其可溶性和抗癌效果.
描述AF装载的DSPE-PEG小粒的物理化学性质,药物释放动力学和体内/体外性能.

主要方法:

阿门托弗拉 (AF) 通过薄膜水化方法被封装到DSPE-PEG小粒中.
分析了微粒特征,包括封装效率,药物负载,颗粒大小和形态.
进行了体外药物释放研究和体内口服生物可用性评估.
在试验室中评估了AF负载小粒的抗瘤疗效.

主要成果:

高封装效率 (98.80%) 和药物负载 (2.96%) 在DSPE-PEG小粒内实现了AF.
由此产生的微粒是球形的,颗粒大小为~26nm,显示AF水溶性增加了412倍.
观察到持续的药物释放,遵循一种基于降解的动力模型.
口服AF的生物可用性增强了3.79倍,而体外抗瘤疗效与自由AF相比显著改善.

结论:

DSPE-PEG微粒有效地提高了阿门托弗拉 (AF) 的水溶性,口服生物可用性和抗癌功效.
这些发现证明了DSPE-PEG菌根的潜力,作为一种可行的药物递送平台,用于改善AF等溶性较差的抗癌剂的治疗结果.

关键词:

在 DSPE-PEG2000 中使用.亚门托弗拉氨酸 (amentoflavone) 是一种它具有抗瘤效果的作用.生物可用性生物可用性

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