Kobryń Justyna, Witkowska Aleksandra, Raszewski Bartosz, Zięba Tomasz, Musiał Witold
Department of Physical Chemistry and Biophysics, Wroclaw Medical University, Borowska 211A, 50-556, Wroclaw, Poland.
Department of Food Storage and Technology, Faculty of Biotechnology and Food Science, Wroclaw University of Environmental and Life Sciences, Chełmońskiego 37, 51-630, Wroclaw, Poland.
Sci Rep. 2025 Jun 2;15(1):19255. doi: 10.1038/s41598-025-88179-x.
The hydrogels with methylene blue (MB), based on selected synthetic and semisynthetic polymers (SP), doped with citrate starch (CS), was evaluated successfully in the terms of MB release from polymeric matrix with prolonged release effect. The hydrophilic matrix in the hydrogel systems affects drug release, systemic absorption and therapeutic effect. The aim of the work was to investigate the use of citrate starch (CS) as an experimental drug carrier for cationic model drug-methylene blue (MB)-in the hydrogel formulation. The native potato starch was modified via esterification and crosslinking with 2.5 and 10.0% (w/w) of citric acid in 120 °C. The hydrogels of methylcellulose (MC), polyacrylic acid (Carbopol 980 NF, C980) and crosspolymer 11 polyacrylate (Aristoflex Velvet, AV) were prepared and doped with native and citrate starches (NS and CS, respectively). The hydrogels without starches were applied as control samples. The release profiles were evaluated in zero-order, first-order, second-order kinetic models, as well as in Higuchi, Korsmeyer-Peppas and Weibull models. The analytical methods as: pH measurements, Fourier transform infrared spectroscopy (ATR-FTIR) as well as scanning electron microscope (SEM), were evaluated. The release kinetics of MB from the MC-based hydrogels matched the Korsmeyer-Peppas and the Higuchi models, while the MB release from C980- and AV-based hydrogels were suited to second-order and the Korsmeyer-Peppas kinetic models. The lowest amount of MB was released after 240 min from AV-based hydrogels with CS addition. In the formulations of C980- and AV-based, both without and containing starch the prolonged MB release was observed, as compared to MC-based formulation. Moreover the citrate starch addition resulted in increased acidity of evaluated hydrogels. The FTIR analysis indicated interactions between the starches and the hydrophilic polymers, as well as between the starches and MB. Moreover, the interactions between MB and C980 and AV were revealed. The most remarkable influence of citrate starches on the MB release was attributed to the content of carboxyl groups in the starches. The studies underlined the validity of the use of the citrate starches, as additives, in synthetic and semisynthetic hydrophilic gels. The possibility to regulate the rate of release of the active substance by appropriate selection of hydrophilic polymer, as well as citrate starch with a selected number of carboxyl groups, may improve a topical and mucosal application of cationic drugs.
基于选定的合成和半合成聚合物（SP）、掺杂柠檬酸盐淀粉（CS）并含有亚甲蓝（MB）的水凝胶，在MB从具有缓释效果的聚合物基质中的释放方面得到了成功评估。水凝胶系统中的亲水性基质会影响药物释放、全身吸收和治疗效果。这项工作的目的是研究在水凝胶制剂中使用柠檬酸盐淀粉（CS）作为阳离子模型药物亚甲蓝（MB）的实验性药物载体。天然马铃薯淀粉通过在120℃下与2.5%和10.0%（w/w）的柠檬酸进行酯化和交联进行改性。制备了甲基纤维素（MC）、聚丙烯酸（卡波姆980 NF，C980）和交联聚合物11聚丙烯酸酯（阿利斯托夫莱克斯天鹅绒，AV）的水凝胶，并分别掺杂天然淀粉和柠檬酸盐淀粉（NS和CS）。不含淀粉的水凝胶用作对照样品。在零级、一级、二级动力学模型以及Higuchi、Korsmeyer-Peppas和Weibull模型中评估释放曲线。评估了如下分析方法：pH测量、傅里叶变换红外光谱（ATR-FTIR）以及扫描电子显微镜（SEM）。基于MC的水凝胶中MB的释放动力学符合Korsmeyer-Peppas和Higuchi模型，而基于C980和AV的水凝胶中MB的释放适合二级和Korsmeyer-Peppas动力学模型。添加CS的基于AV的水凝胶在240分钟后释放的MB量最低。与基于MC的制剂相比，在基于C980和AV的制剂中，无论有无淀粉，均观察到MB的延长释放。此外，添加柠檬酸盐淀粉导致所评估水凝胶的酸度增加。FTIR分析表明淀粉与亲水性聚合物之间以及淀粉与MB之间存在相互作用。此外，还揭示了MB与C980和AV之间的相互作用。柠檬酸盐淀粉对MB释放的最显著影响归因于淀粉中羧基的含量。这些研究强调了在合成和半合成亲水性凝胶中使用柠檬酸盐淀粉作为添加剂的有效性。通过适当选择亲水性聚合物以及具有选定羧基数目的柠檬酸盐淀粉来调节活性物质释放速率的可能性，可能会改善阳离子药物的局部和粘膜应用。
