Brotherton Emma E, Neal Thomas J, Kaldybekov Daulet B, Smallridge Mark J, Khutoryanskiy Vitaliy V, Armes Steven P
Dainton Building, Department of Chemistry, University of Sheffield Brook Hill Sheffield South Yorkshire S3 7HF UK
School of Pharmacy, University of Reading, Whiteknights PO Box 224, Reading Berkshire RG6 6DX UK
Chem Sci. 2022 May 26;13(23):6888-6898. doi: 10.1039/d2sc02074b. eCollection 2022 Jun 15.
A series of thermoresponsive diblock copolymer worm gels is prepared reversible addition-fragmentation chain transfer (RAFT) aqueous dispersion polymerization of 2-hydroxypropyl methacrylate using a water-soluble methacrylic precursor bearing pendent -diol groups. Selective oxidation using an aqueous solution of sodium periodate affords the corresponding aldehyde-functional worm gels. The aldehyde groups are located within the steric stabilizer chains and the aldehyde content can be adjusted by varying the periodate/-diol molar ratio. These aldehyde-functional worm gels are evaluated in terms of their mucoadhesion performance with the aid of a fluorescence microscopy-based assay. Using porcine urinary bladder mucosa as a model substrate, we demonstrate that these worm gels offer a comparable degree of mucoadhesion to that afforded by chitosan, which is widely regarded to be a 'gold standard' positive control in this context. The optimum degree of aldehyde functionality is approximately 30%: lower degrees of functionalization lead to weaker mucoadhesion, whereas higher values compromise the desirable thermoresponsive behavior of these worm gels.
通过使用带有侧链二醇基团的水溶性甲基丙烯酸前体,以可逆加成-断裂链转移(RAFT)水溶液分散聚合法制备了一系列热响应性二嵌段共聚物蠕虫凝胶。使用高碘酸钠水溶液进行选择性氧化,得到相应的醛官能化蠕虫凝胶。醛基位于空间稳定剂链内,醛含量可通过改变高碘酸盐/二醇摩尔比来调节。借助基于荧光显微镜的测定法,对这些醛官能化蠕虫凝胶的粘膜粘附性能进行了评估。以猪膀胱粘膜作为模型底物,我们证明这些蠕虫凝胶提供的粘膜粘附程度与壳聚糖相当,在这种情况下,壳聚糖被广泛认为是“金标准”阳性对照。醛官能化的最佳程度约为30%:较低的官能化程度导致较弱的粘膜粘附,而较高的值会损害这些蠕虫凝胶所需的热响应行为。