Abstract：
Delivering bioactive peptides orally is hampered by poor absorption across the gastrointestinal barrier. Using the walnut-derived peptide PW5, PPKNW, we explored whether coformulation of peptides with absorption enhancer sodium N-[8-(2-hydroxybenzoyl)aminocaprylate] (SNAC) could improve the intestinal absorption of orally-administered bioactive peptides. Herein, the application of SNAC enhanced the absorption efficiency of PW5 in a non-everted gut sac model. Particle size distribution (1 027.8 ± 6.74 nm) and zeta potential (-2.89 ± 0.07 mV) of the PW5-SNAC complex were significantly greater than that of individual PW5 and SNAC. Scanning electron microscopy revealed that SNAC application could aggravate the surface roughness and reduce the compact structure of PW5. It further showed that PW5 and SNAC binds through an endothermic process underpinned by hydrogen bond and van der Waals forces and that SNAC could bound primarily to the internal calyx of PW5. These findings are helpful for the effective delivery of bioactive peptides.
摘要：
口服递送生物活性肽受到穿过胃肠屏障的不良吸收的阻碍。使用核桃衍生肽PW5，PPKNW，我们探讨了肽与吸收促进剂N-[8-（2-羟基苯甲酰基）氨基辛酸钠]（SNAC）的共制剂是否可以改善口服生物活性肽的肠道吸收。在这里，SNAC的应用提高了PW5在非外翻肠囊模型中的吸收效率。PW5-SNAC复合物的粒径分布（1027.8±6.74nm）和ζ电位（-2.89±0.07mV）明显大于单个PW5和SNAC。扫描电子显微镜显示，SNAC的应用可以加剧表面粗糙度并降低PW5的致密结构。它进一步表明，PW5和SNAC通过氢键和范德华力支撑的吸热过程结合，并且SNAC可以主要结合到PW5的内部花萼上。这些发现有助于生物活性肽的有效递送。
