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壳聚糖和 α-纤维素载莫匹罗星局部成膜喷雾的优化、体外特性研究、抗菌研究和伤口愈合活性。

Chitosan and α-cellulose-based mupirocin topical film-forming spray: Optimization, in vitro characterization, antimicrobial studies and wound healing activity.

机构信息

Shobhaben Pratapbhai Patel School of Pharmacy & Technology Management, SVKMs NMIMS, V.L. Mehta Road, Vile Parle (W), Mumbai, Maharashtra 400056, India.

Shobhaben Pratapbhai Patel School of Pharmacy & Technology Management, SVKMs NMIMS, V.L. Mehta Road, Vile Parle (W), Mumbai, Maharashtra 400056, India.

出版信息

Int J Biol Macromol. 2024 Jan;254(Pt 1):127622. doi: 10.1016/j.ijbiomac.2023.127622. Epub 2023 Oct 27.

Abstract

The study aimed to develop a biopolymer-based mupirocin film-forming spray (MUP-FFS) for wound healing using chitosan and α-cellulose. MUP-FFS formulation was optimized by box-Behnken design, wherein the amount of chitosan, glycerol, and microfluidizer cycles showed a significant effect on the drying time and sprayability, but drug release remained unaffected. The optimized MUP-FFS formulation prepared by 13 microfluidizer cycles containing chitosan (0.125 %), glycerol (2.76 %) was quickly sprayable with 235 s drying time. The viscosity, spray uniformity and occlusive potential were found optimum for MUP-FFS. MUP-FFS released 98.066 % of MUP, 2-fold and 4-fold greater than the marketed ointment and MUP-API. The transmission electron microscopy displayed a homogeneous fibrous network, and scanning electron microphotographs showed uniform drug distribution on the MUP-film surface. The antimicrobial study revealed the efficacy of MUP-FFS against S.aureus and E.coli, wherein the former was more susceptible to formulation than the later. MUP-FFS indicated better wound contraction and healing than other groups on 7th and 14th day in rats. On Day-21, MUP-FFS could regress TGF-β1 to a normal level similar to the marketed formulation, which was also reflected in histopathological observations. Therefore, MUP-FFS can be a treatment option for chronic wounds, applied without touch and with minimal mechanical pressure.

摘要

本研究旨在开发一种基于壳聚糖和α-纤维素的莫匹罗星成膜喷雾(MUP-FFS)用于伤口愈合。MUP-FFS 的配方通过 Box-Behnken 设计进行优化,其中壳聚糖、甘油和微射流循环的数量对干燥时间和喷雾性能有显著影响,但药物释放不受影响。通过 13 次微射流循环制备的优化 MUP-FFS 配方,其中壳聚糖(0.125%)、甘油(2.76%)含量较高,干燥时间为 235s,可快速喷雾。MUP-FFS 的粘度、喷雾均匀性和封闭性潜力最佳。MUP-FFS 释放了 98.066%的莫匹罗星,是市售软膏和 MUP-API 的 2 倍和 4 倍。透射电子显微镜显示出均匀的纤维状网络,扫描电子显微镜照片显示药物在 MUP 膜表面均匀分布。抗菌研究表明 MUP-FFS 对金黄色葡萄球菌和大肠杆菌具有功效,其中前者比后者更易受配方影响。在第 7 天和第 14 天,MUP-FFS 在大鼠中的伤口收缩和愈合效果优于其他组。在第 21 天,MUP-FFS 可以将 TGF-β1 回归到与市售制剂相似的正常水平,这也反映在组织病理学观察中。因此,MUP-FFS 可以作为慢性伤口的治疗选择,无需接触和最小机械压力即可应用。

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