Novel biodegradable and pH-sensitive poly(ester amide) microspheres for oral insulin delivery.
Novel biodegradable and pH-sensitive poly(ester amide) microspheres for oral insulin delivery.
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DOI：
10.1002/mabi.201100358
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发表时间：
2012-04
影响因子：
4.6
通讯作者：
Pan He;Zhaohui Tang;Lin Lin-Lin;Mingxiao Deng;X. Pang;Xiu-li Zhuang;Xuesi Chen
中科院分区：
文献类型：
--
作者：
Pan He;Zhaohui Tang;Lin Lin-Lin;Mingxiao Deng;X. Pang;Xiu-li Zhuang;Xuesi Chen
设计、合成并表征了基于双氨基酸的可生物降解且pH敏感的PEAs。胰岛素可以通过油包固体技术负载到PEA微球中，具有高包封率。对PEA微球作为口服胰岛素载体的可行性进行了体内外评价。PEA表面的疏水性亮氨酸基团在PEA微球的pH依赖性释放机制和细胞毒性中起重要作用。链脲佐菌素诱导的糖尿病大鼠口服60 IU/kg的PEA微球后，空腹血糖水平下降至49.4%。这些结果表明PEA微球是一种潜在的胰岛素口服给药新载体。
Biodegradable and pH-sensitive PEAs based on dual amino acids are designed, synthesized, and characterized. Insulin can be loaded into the PEA microspheres by a solid-in-oil-in-oil technique with high encapsulation efficiency. The feasibility of PEA microspheres as oral insulin delivery carriers is evaluated in vitro and in vivo. The hydrophobic leucine groups on PEA seem to play an important role in the pH-dependent release mechanism and cytotoxicity of PEA microspheres. Oral administration of insulin-loaded PEA microspheres to streptozotocin-induced diabetic rats at 60 IU kg(-1) is able to reduce fasting plasma glucose levels to 49.4%. These results indicate that PEA microspheres are potential new vehicles for insulin oral delivery.