人中性粒细胞肽HNP1生物黏附性能的体外评价

In vitro Evaluation on Bioadhesive Property of Human Neutrophil Peptide 1

评价人中性粒细胞肽HNP1(1)的生物黏附性能,探讨其用于修饰眼部递药系统的可行性。采用固相合成技术制备1,考察其与黏蛋白在不同pH溶液中的相互作用,以小动物活体成像观测荧光探针标记的1(1-XS670)在离体兔眼角膜表面的消除。结果表明1能在较宽的pH范围内与黏蛋白相互作用,结合强度在pH 6.0达到最大值(91%),酸性(pH 3.0)条件下二者的结合减弱至58%。荧光标记的1能有效黏附于离体角膜表面,其消除速率显著低于荧光探针对照组(XS670)。因此1是一种新型的生物黏附多肽,在眼部给药方面具有良好的应用前景。

The bioadhesive property of human neutrophil peptide 1 （HNP1, 1） was evaluated to explore the feasibility of developing 1-modified ophthalmic drug delivery system. The peptide was prepared by solid-phase synthesis technology. Interaction between 1 and mucin was evaluated under various pH conditions, and elimination of fluorescent probe-labeled 1 （1-XS670） from isolated rabbit cornea was investigated by an in vivo imaging system. The results showed that 1 could interact with mucin in a wide pH range. The maximum binding percent was observed as 91% at pH 6.0. However, it decreased to 58 % under acidic condition （pH 3.0）. Furthermore, 1-XS670 adhered to the surface of isolated rabbit cornea efficiently, and its elimination rate was significantly slower than that of the fluorescent probe （XS670）. Consequently, 1 was a novel bioadhesive peptide, and was promising in its capacity of developing ophthalmic drug delivery system.