pH-responsive chitosan-mediated spherical mesoporous silica microspheres for high loading and controlled delivery of 5-Fluorouracil

IF 2.4 3区化学 Q3 BIOCHEMISTRY & MOLECULAR BIOLOGY

Carbohydrate Research Pub Date : 2024-07-09 DOI:10.1016/j.carres.2024.109206

Qianqian Zhang , Tong Wan , Guocheng Jin , Shiai Xu

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引用次数: 0

Abstract

The objective of this study is to develop a drug carrier to overcome the inherent drawbacks of 5-Fluorouracil (5-Fu), including low bioavailability, short half-life, and systemic toxicity. In the present work, mesoporous silica nanoparticles (MSNs) capped by chitosan (CS) to encapsulate 5-Fu (5-Fu MSNs/CS) were fabricated by the sol-gel process, ultrasonic impregnation, and emulsion cross-linking. The 5-Fu MSNs/CS microspheres exhibit pH-responsive drug release and remarkable drug encapsulation capacity, as well as perfect sphericity, high specific surface area (680.62 cm²/g), and uniform particle size (2.64 ± 0.05 μm). The drug-loading content and encapsulation efficiency are 14.12 ± 0.53 % and 82.21 ± 2.13 %, respectively. The cumulative release of 5-Fu from MSNs/CS microspheres is fast and sustained at pH 5.0 (89.56 ± 0.97 %) compared to that at pH 7.4 (57.88 ± 0.91 %) in 96 h, and it is Fickian diffusion controlled. In conclusion, the MSNs/CS microspheres prepared in this study could be potential carriers for 5-Fu delivery.

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pH 响应壳聚糖介导的球形介孔二氧化硅微球，用于 5-氟尿嘧啶的高负载和可控给药。

本研究旨在开发一种药物载体，以克服 5-氟尿嘧啶（5-Fu）固有的缺点，包括生物利用度低、半衰期短和全身毒性。本研究采用溶胶-凝胶法、超声浸渍法和乳液交联法制备了壳聚糖（CS）包裹的介孔二氧化硅纳米颗粒（MSNs）来封装 5-Fu（5-Fu MSNs/CS）。所制备的 5-Fu MSNs/CS 微球具有良好的球形度、高比表面积（680.62 cm2/g）和均匀的粒径（2.64 ± 0.05 μm），并具有 pH 值响应性药物释放和显著的药物包封能力。载药量和包封效率分别为 14.12 ± 0.53 % 和 82.21 ± 2.13 %。与 pH 值为 7.4 时（57.88 ± 0.91 %）相比，MSNs/CS 微球在 pH 值为 5.0 时（89.56 ± 0.97 %），5-Fu 在 96 小时内的累积释放速度快且持续，并且是费克扩散控制的。总之，本研究制备的 MSNs/CS 微球可作为潜在的 5-Fu 递送载体。

本文章由计算机程序翻译，如有差异，请以英文原文为准。

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来源期刊

Carbohydrate Research 化学-生化与分子生物学

CiteScore

5.00

自引率

3.20%

发文量

183

审稿时长

3.6 weeks

期刊介绍： Carbohydrate Research publishes reports of original research in the following areas of carbohydrate science: action of enzymes, analytical chemistry, biochemistry (biosynthesis, degradation, structural and functional biochemistry, conformation, molecular recognition, enzyme mechanisms, carbohydrate-processing enzymes, including glycosidases and glycosyltransferases), chemical synthesis, isolation of natural products, physicochemical studies, reactions and their mechanisms, the study of structures and stereochemistry, and technological aspects. Papers on polysaccharides should have a "molecular" component; that is a paper on new or modified polysaccharides should include structural information and characterization in addition to the usual studies of rheological properties and the like. A paper on a new, naturally occurring polysaccharide should include structural information, defining monosaccharide components and linkage sequence. Papers devoted wholly or partly to X-ray crystallographic studies, or to computational aspects (molecular mechanics or molecular orbital calculations, simulations via molecular dynamics), will be considered if they meet certain criteria. For computational papers the requirements are that the methods used be specified in sufficient detail to permit replication of the results, and that the conclusions be shown to have relevance to experimental observations - the authors'' own data or data from the literature. Specific directions for the presentation of X-ray data are given below under Results and "discussion".