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增强型氟康唑负载生物素-谷胱甘肽功能化壳聚糖-g-脯氨酸载体递送至感染性视网膜炎治疗中。

Enhanced systematic delivery of fluconazole-loaded biotin-glutathione functionalized chitosan-g-proline carrier into the infected retinitis treatment.

机构信息

Ophthalmology, Department of Inner Mongolia Chaoju Eye Hospital, Hohhot Inner Mongolia, Hohhot, 010050, China.

Department of Ophthalmology, Affiliated Chenzhou Hospital, The First School of Clinical Medicine, Southern Medical University, The First People's Hospital of Chenzhou), Chenzhou, Hunan, 423000, China.

出版信息

BMC Ophthalmol. 2024 Jan 30;24(1):48. doi: 10.1186/s12886-024-03305-z.

Abstract

BACKGROUND

The polymer-based facile and effective drug carrier approach was developed to treat superficial fungal infected retinopathy infections.

METHODS

Here, biotin-glutathione (B-GHS) functionalized with chitosan grafted proline (CS-g-P) moieties were fabricated with the loading of fluconazole (FLZ) for the treatment of retinopathy. FT-IR and XRD techniques were used to characterize chemical structural and phase changes of the prepared carriers The SEM results show that the sphere morphology with interconnection particle nature.

RESULTS

The particle diameter was found as ~ 6.5 and ~ 8.6 nm for CS-g-P/B-GHS and FLZ-loaded CS-g-P/B-GHS carriers, respectively. The negative surface charge was found as the values of CS-g-P/B-GHS and FLZ-loaded CS-g-P/B-GHS, such as -20.7 mV and - 32.2 mV, from zeta potential analysis. The in-vitro FLZ releases from the CS-g-P/B-GHS were investigated at pH 7.4 (PBS) as the tear fluid environment, and it was observed at 85.02% of FLZ release in 8 h reaction time. The sustained release was observed, leading to the necessity for prolonged therapeutic effects. The antifungal effect of the carrier was studied by the minimum inhibitory concentration (MIC) and the percentage inhibition of viable fungal count against Candida albicans, and it observed 81.02% of the zone of inhibition by the FLZ carrier.

CONCLUSION

FLZ-loaded CS-g-P/B-GHS carrier could inhibit the biofilm formation in a concentration-dependent inhibition. Hence, A novel FLZ/B-GHS-CS-g-P carrier is a hopeful approach for effectively treating superficial fungal contaminations of the retina region.

摘要

背景

本研究开发了基于聚合物的简便有效药物载体方法,用于治疗浅表真菌感染性视网膜病变。

方法

在这里,制备了生物素-谷胱甘肽(B-GHS)功能化接枝脯氨酸的壳聚糖(CS-g-P)部分,并负载氟康唑(FLZ)用于治疗视网膜病变。傅里叶变换红外和 X 射线衍射技术用于表征所制备载体的化学结构和相变化。SEM 结果表明,具有互联颗粒性质的球体形态。

结果

发现 CS-g-P/B-GHS 和载有 FLZ 的 CS-g-P/B-GHS 载体的粒径分别约为 6.5 和 8.6nm。通过zeta 电位分析,发现 CS-g-P/B-GHS 和载有 FLZ 的 CS-g-P/B-GHS 的表面带负电荷,分别为-20.7 mV 和-32.2 mV。在 pH 7.4(PBS)作为泪液环境的体外研究中,观察到 CS-g-P/B-GHS 中 8 小时反应时间内释放了 85.02%的 FLZ。观察到持续释放,导致需要延长治疗效果。通过最小抑菌浓度(MIC)和对白色念珠菌活菌计数的抑制百分比研究了载体的抗真菌作用,观察到 FLZ 载体的抑菌环为 81.02%。

结论

FLZ 负载的 CS-g-P/B-GHS 载体可以在浓度依赖性抑制下抑制生物膜的形成。因此,新型 FLZ/B-GHS-CS-g-P 载体有望有效治疗视网膜区域的浅表真菌感染。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/a740/10826221/ff72a50d13cb/12886_2024_3305_Fig1_HTML.jpg

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