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Box-Behnken设计辅助优化与表征用于同时局部递送抗坏血酸和甲硝唑的壳聚糖膜

Box-Behnken Design Assisted Optimization and Characterization of Chitosan Film for Simultaneous Topical Delivery of Ascorbic Acid and Metronidazole.

作者信息

Khan Bilawal, Kraisit Pakorn, Santhan Supaporn, Hirun Namon

机构信息

Division of Pharmaceutical Sciences, Faculty of Pharmacy, Thammasat University, Pathumthani 12120, Thailand.

Thammasat University Research Unit in Smart Materials and Innovative Technology for Pharmaceutical Applications (SMIT-Pharm), Faculty of Pharmacy, Thammasat University, Pathumthani 12120, Thailand.

出版信息

Pharmaceutics. 2025 Apr 24;17(5):562. doi: 10.3390/pharmaceutics17050562.

DOI:10.3390/pharmaceutics17050562
PMID:40430855
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC12115047/
Abstract

The objective of this study was to develop chitosan films plasticized with glycerol for the topical delivery of ascorbic acid and metronidazole. The films were prepared using a casting technique in which an aqueous ascorbic acid solution served as the solvent, eliminating the need for additional mineral or organic acids. The influence of compositions on film characteristics-specifically mechanical properties and surface pH-was examined, and an optimized formulation was identified using a Box-Behnken design-response surface methodology. Relevant characterization techniques and in vitro evaluations were conducted to assess the properties and performance of the optimized film formulation. Results showed that both glycerol and ascorbic acid contributed to the plasticization of the films. Fourier-transform infrared spectroscopic analysis of the optimized film revealed the formation of chitosan ascorbate and interactions between chitosan and glycerol. In addition, the thermogram and powder X-ray diffractogram demonstrated alterations in the thermal behavior and crystallinity of the embedded bioactive compounds. The developed film possessed the preferred swelling capacity. Moreover, in vitro release studies revealed a co-release pattern, delivering both bioactive compounds simultaneously. These findings suggest that the prepared chitosan-based film could serve as a promising platform for topical delivery.

摘要

本研究的目的是开发用甘油增塑的壳聚糖薄膜,用于抗坏血酸和甲硝唑的局部给药。这些薄膜采用流延技术制备,其中抗坏血酸水溶液用作溶剂,无需额外的无机酸或有机酸。研究了组成对薄膜特性(特别是机械性能和表面pH值)的影响,并使用Box-Behnken设计-响应面法确定了优化配方。进行了相关的表征技术和体外评估,以评估优化薄膜配方的性能。结果表明,甘油和抗坏血酸都有助于薄膜的增塑。对优化薄膜的傅里叶变换红外光谱分析表明,形成了抗坏血酸壳聚糖盐以及壳聚糖与甘油之间的相互作用。此外,热重曲线和粉末X射线衍射图显示了包埋生物活性化合物的热行为和结晶度的变化。所制备的薄膜具有理想的溶胀能力。此外,体外释放研究显示出共同释放模式,可同时递送两种生物活性化合物。这些发现表明,所制备的基于壳聚糖的薄膜可作为一种有前景的局部给药平台。

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