Escuela de Química, Facultad de Ciencias, Universidad Industrial de Santander, Cra 27 # calle 9 (CP680002) Bucaramanga, Colombia. Departamento de Química, Universidad Nacional de Colombia, Cra 30 # 45-03, 111321 Bogotá, Colombia.
Nanotechnology. 2017 Mar 1;28(13):135102. doi: 10.1088/1361-6528/aa5f63.
Nanocarrier systems are currently being developed for peptide, protein and gene delivery to protect them in the blood circulation and in the gastrointestinal tract. Polylactic acid (PLA) and poly(lactic-co-glycolic) acid (PLGA) nanoparticles loaded with a new antimicrobial GIBIM-P5S9K peptide were obtained by the double emulsion solvent extraction/evaporation method. PLA- and PLGA-NPs were spherical with sizes between 300 and 400 nm for PLA and 200 and 300 nm for PLGA and <0.3 polydispersity index as determined by dynamic light scattering and scanning electron microscopy), having the zeta potential of >20 mV. The peptide-loading efficiency of PLA-NP and PLGA-NPs was 75% and 55%, respectively. PLA- and PLGA-NPs released around 50% of this peptide over 8 h. In 10% human sera the size of peptide loaded PLA- and PLGA-NPs increased between 25.2% and 39.3%, the PDI changed from 3.2 to 5.1 and the surface charge from -7.15 to 14.6 mV. Both peptide loaded PLA- and PLGA-NPs at 0.5 μM peptide concentration inhibited the growth of Escherichia coli O157:H7 (E. coli O157:H7), methicillin-resistant Staphylococcus aureus (MRSA) and Pseudomonas. aeruginosa (P. aeruginosa). In contrast, free peptide inhibited at 10 μM but did not inhibit at 0.5 and 1 μM. These PLA- and PLGA-NPs presented <10% hemolysis indicating that they are hemocompatible and promising for delivery and protection system of GIBIM-P5S9K peptide.
纳米载体系统目前正在被开发用于肽、蛋白质和基因的递送来保护它们在血液循环和胃肠道中的稳定性。通过双乳液溶剂萃取/蒸发法得到了载有新型抗菌 GIBIM-P5S9K 肽的聚乳酸（PLA）和聚（乳酸-共-乙醇酸）（PLGA）纳米粒。PLA 和 PLGA 纳米粒为球形，粒径分别在 300-400nm 和 200-300nm 之间，通过动态光散射和扫描电子显微镜测定的多分散指数 <0.3，zeta 电位 >20mV。PLA-NP 和 PLGA-NP 的载药效率分别为 75%和 55%。PLA 和 PLGA-NP 在 8 小时内分别释放约 50%的肽。在 10%的人血清中，载有肽的 PLA 和 PLGA-NP 的粒径增加了 25.2%-39.3%，PDI 从 3.2 变为 5.1，表面电荷从-7.15 变为 14.6mV。在 0.5μM 肽浓度下，载有肽的 PLA 和 PLGA-NP 均能抑制大肠杆菌 O157:H7（E. coli O157:H7）、耐甲氧西林金黄色葡萄球菌（MRSA）和铜绿假单胞菌（P. aeruginosa）的生长。相比之下，游离肽在 10μM 时抑制作用明显，但在 0.5μM 和 1μM 时没有抑制作用。这些 PLA 和 PLGA-NP 的溶血率 <10%，表明它们具有血液相容性，有望成为 GIBIM-P5S9K 肽的递药和保护系统。
