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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。
To evaluate the bioadhesive properties of human neutrophil peptide HNP1 (1), and to explore the feasibility of using it to modify the ophthalmic delivery system. Preparation of 1 by solid-phase synthesis technology to investigate its interaction with mucins in different pH solutions, small animal live imaging observed fluorescent probe labeled 1 (1-XS670) in isolated rabbit corneal surface elimination. The results showed that 1 could interact with mucins over a wide range of pH. The binding strength decreased to 58% at pH 6.0 (91%) and acidic pH (pH 3.0). Fluorescently labeled 1 effectively adhered to the isolated corneal surface with a significantly lower elimination rate than the fluorescent probe control group (XS670). So 1 is a novel bioadhesive peptide, which has a good prospect in the field of ophthalmic administration.