聚己内酯-聚乙二醇-聚己内酯温敏三嵌段共聚物注射形成凝胶中生长激素的释放评价

Release Evaluation of Growth Hormone from an Injectable Forming Gel Using PCL-PEG-PCL Thermosensitive Triblock.

机构信息

Targeted Drug Delivery Research Center, Pharmaceutical Technology Institute, Mashhad University of Medical Sciences, Mashhad, Iran.

Department of Pharmaceutics, School of Pharmacy, Mashhad University of Medical Sciences, Mashhad, Iran.

出版信息

Curr Drug Deliv. 2020;17(2):174-183. doi: 10.2174/1567201817666200120120105.

DOI:10.2174/1567201817666200120120105

PMID:31987020

Abstract

OBJECTIVE

An injectable long acting In-Situ Forming Gel (ISFG) of human Growth Hormone (hGH) was prepared by using triblock PCL-PEG-PCL (Mw 1500-1500-1500). Ring-Opening Polymerization (ROP) of triblock using microwave was applied.

METHODS

The BCA protein assay Kit was used to determine the concentration of hGH in the in-vitro release medium. Finally, Sodium Dodecyl Sulfate-Polyacrylamide Gel Electrophoresis (SDS-PAGE) tests and Circular Dichroism (CD) spectrum were done to approve the stability of released hGH. The result of ROP demonstrated that the proportion of PCL to PEG accorded with the initial molar ratio of the monomers. The cross-section of the Surface Electron Microscopy (SEM) indicated the porous framework of the hydrogel could load the drug into its tridimensional matrixes structure. There is the low initial burst release of hGH from the supramolecular hydrogel.

RESULTS

The maximum in-vitro release of hGH was 71.2 % ± 1.5 that were due to hGH degrading after this time (21 days). The CD spectrum and SDS-PAGE results confirmed the stability of hGH during invitro release evaluation.

CONCLUSION

The results suggest that the sustained-release formulation using PCL-PEG-PCL can be applied to control the release of hGH.

摘要

目的

通过使用三嵌段聚己内酯-聚乙二醇-聚己内酯（MW1500-1500-1500）制备了可注射长效原位形成凝胶（ISFG）的人生长激素（hGH）。应用微波进行三嵌段开环聚合（ROP）。

方法

使用 BCA 蛋白测定试剂盒测定体外释放介质中 hGH 的浓度。最后，进行十二烷基硫酸钠-聚丙烯酰胺凝胶电泳（SDS-PAGE）测试和圆二色性（CD）光谱测试，以验证释放的 hGH 的稳定性。ROP 的结果表明，PCL 与 PEG 的比例与单体的初始摩尔比相符。表面电子显微镜（SEM）的横截面表明，水凝胶的多孔骨架可以将药物负载到其三维基质结构中。超分子水凝胶中 hGH 的初始突释较低。