Study on the Influencing Factors of Hypoglycemic Effect of Folate Targeted Polymersomes Encapsulating Insulin.
Study on the Influencing Factors of Hypoglycemic Effect of Folate Targeted Polymersomes Encapsulating Insulin.
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叶酸靶向封装胰岛素聚合物囊泡降血糖影响因素的研究。
DOI：
10.1016/j.xphs.2020.11.042
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发表时间：
2020-12
期刊：
影响因子：
--
通讯作者：
Xiong Xiang Yuan
中科院分区：
文献类型：
--
作者：
Chen Dao Ge;Zhao Cheng Wu;Gong Yan Chun;Li Zi Ling;Li Yu Ping;Xiong Xiang Yuan
目的研究叶酸浓度对叶酸靶向聚合物囊泡作为口服胰岛素载体降血糖作用的影响。研究不同质量比的d-α-生育酚聚乙二醇1000琥珀酸酯（TPGS）对FA靶向聚合物囊泡降血糖作用的影响。研究了不同FA含量的FA靶向聚合物囊泡在不同介质中的体外胰岛素释放实验。检测了它们在Caco-2细胞中的定量细胞摄取。还用糖尿病大鼠研究了FA靶向聚合物囊泡的体内降血糖活性。结果在四种不同FA摩尔含量的胰岛素载FA靶向聚合物囊泡中，FA摩尔含量为10%的胰岛素载FA聚合物囊泡（胰岛素载10%FA-Ps）的细胞摄取最高，降糖效果最好。此外，FA-Ps/TPGS 5：1混合聚合物囊泡的细胞摄取率和降血糖效果均优于另外两种加入TPGS的胰岛素聚合物囊泡。
PurposeTo study the effects of the density of folic acid (FA) on the hypoglycemic ability of FA-targeted polymersomes as oral insulin carriers. Also to study the change of the hypoglycemic effect of FA-targeted mixed polymersomes added with various mass ratio ofd-α-tocopherol polyethylene glycol 1000 succinate (TPGS).MethodsThe FA-targeted polymersomes with different FA molar contents were prepared. The in vitro insulin release experiments in different media for FA-targeted polymersomes with various FA contents were studied. Their quantitative cellular uptake in Caco-2 cells was examined. The in vivo hypoglycemic activity of FA-targeted polymersomes was also studied with diabetic rats. The polymersomes with the optimal FA molar content was chosen to prepare mixed polymersomes with various TPGS contents.ResultsAmong insulin-loaded FA-targeted polymersomes with four different FA molar contents, insulin-loaded polymersomes with 10% FA molar content (insulin-loaded 10%FA-Ps) showed the hightest cellular uptake and the best hypoglycemic response. In addition, the insulin-loaded FA-Ps/TPGS5:1 mixed polymersomes exhibited higher cellular uptake and better hypoglycemic response than the other two insulin-loaded mixed polymersomes adding TPGS did.ConclusionsFA-Ps/TPGS5:1 could be a promising formulation for the oral administration of insulin.
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