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胰岛素从叶酸-胰岛素复合纳米颗粒中的控释。

Controlled release of insulin from folic acid-insulin complex nanoparticles.

作者信息

Gupta Rajat, Mohanty Sanat

机构信息

Department of Chemical Engineering, Indian Institute of Technology Delhi, New Delhi, 110016, India.

Department of Chemical Engineering, Indian Institute of Technology Delhi, New Delhi, 110016, India.

出版信息

Colloids Surf B Biointerfaces. 2017 Jun 1;154:48-54. doi: 10.1016/j.colsurfb.2017.03.002. Epub 2017 Mar 3.

DOI:10.1016/j.colsurfb.2017.03.002
PMID:28288342
Abstract

Associative interactions between folic acid and proteins are well known. This work leverages these interactions to engineer folic acid nanoparticles for controlled release of insulin during diabetes therapy. The insulin-loaded folic acid nanoformulation is synthesized during this study to achieve better insulin loading and encapsulation than previous strategies. The maximum insulin loading in the FA particles was kept at 6mg with less than 10% insulin loss during the synthesis process which is significantly better compare to previous strategies. The folic acid nanoparticles of 50-150nm size are further characterized in the present study. The release behaviour of insulin from the nanoparticles has been studied to quantify released insulin and folic acid with time using high performance liquid chromatography. Insulin release results suggest that more than 90% of the insulin is encapsulated and released within 24h from folic acid nanoparticles. The analysis of folic acid release along with insulin release indicates that the particles are formed by folic acid-insulin complexation at the molecular level. The release of insulin from nanoparticles is controllable with the change in the crosslinking salt concentration as well as the amount of folic acid loaded during particle synthesis. These results prove that folic acid nanocarriers are capable to control the release of therapeutic proteins.

摘要

叶酸与蛋白质之间的缔合相互作用是众所周知的。这项工作利用这些相互作用来设计叶酸纳米颗粒,用于糖尿病治疗期间胰岛素的控释。在本研究中合成了负载胰岛素的叶酸纳米制剂,以实现比以前的策略更好的胰岛素负载和包封。FA颗粒中的最大胰岛素负载量保持在6mg,在合成过程中胰岛素损失小于10%,这与以前的策略相比有显著改善。本研究进一步对尺寸为50 - 150nm的叶酸纳米颗粒进行了表征。使用高效液相色谱法研究了纳米颗粒中胰岛素的释放行为,以量化随时间释放的胰岛素和叶酸。胰岛素释放结果表明,超过90%的胰岛素被包封在叶酸纳米颗粒中,并在24小时内释放。对叶酸释放与胰岛素释放的分析表明,颗粒是通过叶酸与胰岛素在分子水平上的络合形成的。纳米颗粒中胰岛素的释放可通过交联盐浓度的变化以及颗粒合成过程中叶酸负载量的变化来控制。这些结果证明叶酸纳米载体能够控制治疗性蛋白质的释放。

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