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pH-Triggered nanostructural transformations in antimicrobial peptide/oleic acid self-assemblies†
Biomaterials Science ( IF 6.6 ) Pub Date : 2018-01-15 00:00:00 , DOI: 10.1039/c7bm00929a
Mark Gontsarik 1, 2, 3, 4, 5 , Mahsa Mohammadtaheri 1, 2, 3, 4, 5 , Anan Yaghmur 6, 7, 8, 9, 10 , Stefan Salentinig 1, 2, 3, 4, 5
Affiliation  

The delivery of poorly water-soluble antimicrobial peptides (AMPs) that are sensitive to degradation is a major challenge in the pharmaceutical field. In this study, we design and characterize a pH-sensitive nanocarrier with the potential for delivery of AMPs and their protection from degradation. These nanobiointerfaces are prepared through the self-assembly of oleic acid (OA) with the human cathelicidin LL-37 in excess water. Advanced experimental methods including synchrotron small angle X-ray scattering, cryogenic transmission electron microscopy, and dynamic light scattering were used to characterize the OA/LL-37 self-assemblies and their structural alterations in response to changes in pH and composition. Experimental findings reveal colloidal transformations from normal emulsions via micellar cubosomes and hexosomes to vesicles upon increasing the pH from 6.0 to 8.0 at a LL-37 content around 10 wt% relative to OA. Increasing the LL-37 content to 30 wt% in OA led to diminishing of micellar cubosomes and hexosomes in this narrow pH range, favoring the formation of micelles and vesicles of various shapes and sizes. Upon increasing the pH, with the strongest effect around pH 7.5, charge repulsions among the gradually deprotonating carboxylic groups of OA modified the geometric packing of the molecules, significantly affecting the nanostructure. These detailed insights into the formation of this unique family of nanobiointerfaces and their tunable structural features may contribute to the rational design of pH-responsive antimicrobial systems for the delivery of peptides, particularly poorly water-soluble AMPs.

中文翻译:

pH触发的抗菌肽/油酸自组装中的纳米结构转变

对降解敏感的水溶性差的抗微生物肽(AMP)的递送是制药领域的主要挑战。在这项研究中,我们设计和表征了对pH敏感的纳米载体,具有传递AMP的潜力及其对降解的保护作用。这些纳米生物界面是通过油酸(OA)与人cathelicidin LL-37在过量水中的自组装而制备的。先进的实验方法包括同步加速器小角度X射线散射,低温透射电子显微镜和动态光散射来表征OA / LL-37自组装及其响应pH和组成变化的结构变化。实验结果表明,普通乳状液通过在相对于OA约10 wt%的LL-37含量将pH从6.0增加到8.0时,胶束立方体和六体变为囊泡。在此狭窄的pH范围内,将OA中的LL-37含量提高至30 wt%导致胶束立方脂质体和六脂质体的减少,有利于形成各种形状和大小的胶束和囊泡。随着pH的增加,OA逐渐脱质子化的羧基之间的电荷排斥会在pH 7.5附近产生最强的影响,从而改变了分子的几何堆积,从而显着影响了纳米结构。对这种独特的纳米生物界面家族的形成及其可调节的结构特征的这些详细见解,可能有助于合理设计pH响应型抗菌系统以输送肽,特别是水溶性较差的AMP。
更新日期:2018-01-15
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