Data from: Amphotericin B-conjugated poly-peptide hydrogels as a novel strategy for fungal infections

The present work is focused on design and development of novel Amphotericin B-conjugated biocompatible and biodegradable poly-peptide hydrogels to improve the antifungal activity. Using three kinds of promoting self-assembly groups (2-naphthalene acetic acid, Naproxen and Dexamethasone) and poly-peptide sequence (Phe-Phe-Asp-Lys-Tyr, FFDKY), we successfully synthesized the Nap-FFDK (AmB) Y gels, Npx-FFDK (AmB) Y gels and Dex-FFDK (AmB) Y gels. The Amphotericin B-conjugated hydrogelators are highly soluble in different aqueous solutions. The Cryo-transmission electron microscopy (TEM) and scanning electron microscopy (SEM) micrographs of hydrogels afford nanofibers with width of 20~50 nm. Powder X-ray diffraction (PXRD) analyses demonstrate that the crystalline structure of the AmB and Dex are changed into amorphous structure after formation of hydrogels. Circular dichroism (CD) spectra of the solution of blank carriers and the corresponding drug deliveries further help elucidate the molecular arrangement in gel phase, indicating the existence of turn features. The in vitro drug releases suggest that the Amphotericin B-conjugated hydrogels are suitable as drug-controlled release vehicles for hydrophobic drug. The antifungal effect of AmB-conjugated hydrogels significantly exhibits the antifungal activity against Candida albicans. The results of present study indicated that the Amphotericin B-conjugated hydrogels are suitable carriers for poorly water soluble drugs and for enhancement of therapeutic efficacy of antifungal drugs.

本研究聚焦于新型两性霉素B（Amphotericin B）偶联的生物相容性可降解多肽水凝胶的设计与开发，旨在提升其抗真菌活性。本研究选用三种促自组装基团（2-萘乙酸、萘普生、地塞米松）以及多肽序列（苯丙氨酸-苯丙氨酸-天冬氨酸-赖氨酸-酪氨酸，Phe-Phe-Asp-Lys-Tyr，FFDKY），成功合成了Nap-FFDK(AmB)Y凝胶、Npx-FFDK(AmB)Y凝胶与Dex-FFDK(AmB)Y凝胶。该两性霉素B偶联水凝胶因子在多种水溶液中均具有优异的溶解性。水凝胶的冷冻透射电子显微镜（Cryo-transmission electron microscopy，Cryo-TEM）与扫描电子显微镜（scanning electron microscopy，SEM）图像显示，其呈现宽度为20~50 nm的纳米纤维结构。粉末X射线衍射（Powder X-ray diffraction，PXRD）分析结果表明，两性霉素B与地塞米松的晶体结构在水凝胶形成后转变为无定形结构。空白载体与对应载药体系的圆二色光谱（Circular dichroism，CD）进一步阐明了凝胶相中的分子排列特征，表明体系中存在转角结构。体外药物释放实验结果表明，该两性霉素B偶联水凝胶可作为疏水药物的控释载体。AmB偶联水凝胶的抗真菌效果显著，对白色念珠菌（Candida albicans）具有良好的抗真菌活性。本研究结果证实，两性霉素B偶联水凝胶可作为水溶性较差药物的递送载体，同时可提升抗真菌药物的治疗效能。