Tawfeek Hesham M, Khidr Sayed H, Samy Eman M, Ahmed Sayed M, Gaskell Elsie E, Hutcheon Gillian A
School of Pharmacy and Biomolecular Sciences, Liverpool John Moores University , Liverpool , UK and.
Drug Dev Ind Pharm. 2014 Sep;40(9):1213-22. doi: 10.3109/03639045.2013.814060. Epub 2013 Jul 15.
Abstract Poly(glycerol adipate-co-ω-pentadecalactone) (PGA-co-PDL) was previously evaluated for the colloidal delivery of α-chymotrypsin. In this article, the effect of varying polymer molecular weight (MW) and chemistry on particle size and morphology; encapsulation efficiency; in vitro release; and the biological activity of α-chymotrypsin (α-CH) and lysozyme (LS) were investigated. Microparticles were prepared using emulsion solvent evaporation and evaluated by various methods. Altering the MW or monomer ratio of PGA-co-PDL did not significantly affect the encapsulation efficiency and overall poly(1,3-propanediol adipate-co-ω-pentadecalactone) (PPA-co-PDL) demonstrated the highest encapsulation efficiency. In vitro release varied between polymers, and the burst release for α-CH-loaded microparticles was lower when a higher MW PGA-co-PDL or more hydrophobic PPA-co-PDL was used. The results suggest that, although these co-polyesters could be useful for protein delivery, little difference was observed between the different PGA-co-PDL polymers and PPA-co-PDL generally provided a higher encapsulation and slower release of enzyme than the other polymers tested.
摘要 聚（己二酸甘油酯 - 共 - ω - 十五内酯）（PGA - co - PDL）先前已被评估用于α - 胰凝乳蛋白酶的胶体递送。在本文中，研究了聚合物分子量（MW）和化学组成的变化对粒径和形态、包封效率、体外释放以及α - 胰凝乳蛋白酶（α - CH）和溶菌酶（LS）生物活性的影响。使用乳液溶剂蒸发法制备微粒，并通过各种方法进行评估。改变PGA - co - PDL的分子量或单体比例对包封效率没有显著影响，总体而言聚（1,3 - 丙二醇己二酸酯 - 共 - ω - 十五内酯）（PPA - co - PDL）表现出最高的包封效率。聚合物之间的体外释放情况各不相同，当使用较高分子量的PGA - co - PDL或更疏水的PPA - co - PDL时，负载α - CH的微粒的突释较低。结果表明，尽管这些共聚酯可用于蛋白质递送，但在不同的PGA - co - PDL聚合物之间观察到的差异不大，并且与测试的其他聚合物相比，PPA - co - PDL通常具有更高的酶包封率和更慢的释放速度。
