Aldilla Vina R, Martin Adam D, Nizalapur Shashidhar, Marjo Christopher E, Rich Anne M, Ho Kitty K K, Ittner Lars M, Black David StC, Thordarson Pall, Kumar Naresh
School of Chemistry, UNSW, Sydney, NSW 2052, Australia.
J Mater Chem B. 2018 Oct 14;6(38):6089-6098. doi: 10.1039/c8tb01290c. Epub 2018 Sep 10.
In this study, we report the synthesis of glyoxylamide peptide-mimics as self-assembled gels with well-defined molecular structures for topical delivery of ciprofloxacin (CIP). The glyoxylamide peptide mimics successfully formed hydrogels with critical gel concentrations of 0.02-0.08% (w/v). The mechanical strength, secondary structure, and fiber morphology of these hydrogels can be modulated by varying the N-substituent of the ring-opened isatins. The synthesised hydrogel exhibited a high loading capacity of CIP (40% (w/w)) and a sustained release profile. The CIP-loaded hydrogels were able to release CIP for more than 15 days and the released solution was shown to retain activity against Gram-positive and Gram-negative bacteria. In addition, the hydrogels formed showed low toxicity against Cos7 cells.
在本研究中，我们报道了乙二醛酰胺肽模拟物的合成，其作为具有明确分子结构的自组装凝胶用于环丙沙星（CIP）的局部递送。乙二醛酰胺肽模拟物成功形成了临界凝胶浓度为0.02 - 0.08%（w/v）的水凝胶。通过改变开环异吲哚酮的N - 取代基，可以调节这些水凝胶的机械强度、二级结构和纤维形态。合成的水凝胶表现出较高的CIP负载量（40%（w/w））和缓释特性。负载CIP的水凝胶能够释放CIP超过15天，并且释放的溶液对革兰氏阳性菌和革兰氏阴性菌均保持活性。此外，形成的水凝胶对Cos7细胞显示出低毒性。
