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壳聚糖衍生物基薄膜作为 pH 敏感型药物传递系统,具有增强的抗氧化和抗菌性能。

Chitosan derivatives-based films as pH-sensitive drug delivery systems with enhanced antioxidant and antibacterial properties.

机构信息

Laboratory of Enzyme Engineering and Microbiology, National School of Engineering of Sfax (ENIS), University of Sfax, P.O. Box 1173, Sfax 3038, Tunisia.

Department of Chemistry in Pharmaceutical Science, Faculty of Pharmacy, Pluridisciplinar Institute, Complutense University of Madrid, 28040 Madrid, Spain.

出版信息

Int J Biol Macromol. 2021 Jul 1;182:730-742. doi: 10.1016/j.ijbiomac.2021.04.014. Epub 2021 Apr 6.

DOI:10.1016/j.ijbiomac.2021.04.014
PMID:33836191
Abstract

The purpose of this study was to develop and characterize chitosan (Ch)-based films incorporated with varying molecular weight (Mw) and acetylation degree (AD) chitosan-depolymerization-products (CDP), to be applied as drug delivery materials. As compared to Ch-film, optical and antioxidant potentials of Ch/CDP-based films were improved, particularly using low Mw and AD-CDP. Whereas, films water resistance, mechanical and antibacterial properties increased as CDP-Mw increased and AD decreased. For the thermal and swelling behaviors, better values were obtained using higher Mw and AD-CDP. Further, to assess their in vitro ciprofloxacin (CFX)-release behavior, loaded-CFX Ch/CDP-based films, crosslinked using glutaraldehyde, were prepared. Expect of elongation at break, crosslinked CFX-loaded films showed increased optical, water resistance, tensile strength and thermal properties, as compared to unloaded films. The CFX-release profiles indicated that a slower and sustained release was observed, particularly when using lower Mw and AD-CDP, and mainly for the crosslinked films during 48 h. These films can release CFX for up to 54% in 6 and 24 h, at pH 1.2 and 7.4, respectively. Through this study, novel biodegradable, swellable and pH-sensitive crosslinked Ch/CDP-based films may be considered as suitable and promising drug delivery systems.

摘要

本研究旨在开发和表征壳聚糖(Ch)基膜,其中掺入了不同分子量(Mw)和乙酰化度(AD)的壳聚糖解聚产物(CDP),以用作药物递送材料。与 Ch 膜相比,Ch/CDP 基膜的光学和抗氧化性能得到了改善,特别是使用低 Mw 和 AD-CD P 时。然而,随着 CDP-Mw 的增加和 AD 的降低,膜的耐水性、机械性能和抗菌性能得到了提高。对于热和溶胀行为,使用较高的 Mw 和 AD-CD P 可获得更好的值。此外,为了评估它们在体外环丙沙星(CFX)释放行为,使用戊二醛交联制备了载有 CFX 的 Ch/CDP 基膜。与未载药的膜相比,交联的载有 CFX 的膜在断裂伸长率降低的情况下,显示出更高的光学、耐水性、拉伸强度和热性能。CFX 释放曲线表明,观察到较慢和持续的释放,特别是使用较低 Mw 和 AD-CD P 时,并且在 48 小时内主要是交联膜。这些膜可以在 6 和 24 小时内分别在 pH 1.2 和 7.4 下释放高达 54%的 CFX。通过这项研究,新型可生物降解、溶胀和 pH 敏感的交联 Ch/CDP 基膜可被认为是合适且有前途的药物递送系统。

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