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用于结肠靶向给药的pH敏感水凝胶的设计;表征与体外评价。

Designing of pH-Sensitive Hydrogels for Colon Targeted Drug Delivery; Characterization and In Vitro Evaluation.

作者信息

Suhail Muhammad, Shao Yu-Fang, Vu Quoc Lam, Wu Pao-Chu

机构信息

School of Pharmacy, Kaohsiung Medical University, Kaohsiung City 80708, Taiwan.

Department of Biomedical Science and Environmental Biology, Kaohsiung Medical University, Kaohsiung City 80708, Taiwan.

出版信息

Gels. 2022 Mar 3;8(3):155. doi: 10.3390/gels8030155.

Abstract

In the current research work, pH-sensitive hydrogels were prepared via a free radical polymerization technique for the targeted delivery of 5-aminosalicylic acid to the colon. Various proportions of chitosan, β-Cyclodextrin, and acrylic acid were cross-linked by ethylene glycol dimethacrylate. Ammonium persulfate was employed as an initiator. The development of a new polymeric network and the successful encapsulation of the drug were confirmed by Fourier transform infrared spectroscopy. Thermogravimetric analysis indicated high thermal stability of the hydrogel compared to pure chitosan and β-Cyclodextrin. A rough and hard surface was revealed by scanning electron microscopy. Similarly, the crystallinity of the chitosan, β-Cyclodextrin, and fabricated hydrogel was evaluated using powder X-ray diffraction. The swelling and drug release studies were performed in both acidic and basic medium (pH 1.2 and 7.4, respectively) at 37 °C. High swelling and drug release was observed at pH 7.4 as compared to pH 1.2. The increased incorporation of chitosan, β-Cyclodextrin, and acrylic acid led to an increase in porosity, swelling, loading, drug release, and gel fraction of the hydrogel, whereas a decrease in sol fraction was observed. Thus, we can conclude from the results that a developed pH-sensitive network of hydrogel could be employed as a promising carrier for targeted drug delivery systems.

摘要

在当前的研究工作中,通过自由基聚合技术制备了pH敏感水凝胶,用于将5-氨基水杨酸靶向递送至结肠。壳聚糖、β-环糊精和丙烯酸的不同比例通过乙二醇二甲基丙烯酸酯交联。过硫酸铵用作引发剂。傅里叶变换红外光谱证实了新聚合物网络的形成以及药物的成功包封。热重分析表明,与纯壳聚糖和β-环糊精相比,水凝胶具有较高的热稳定性。扫描电子显微镜显示表面粗糙且坚硬。同样,使用粉末X射线衍射评估壳聚糖、β-环糊精和制备的水凝胶的结晶度。在37℃下于酸性和碱性介质(分别为pH 1.2和7.4)中进行溶胀和药物释放研究。与pH 1.2相比,在pH 7.4下观察到高溶胀和药物释放。壳聚糖、β-环糊精和丙烯酸掺入量的增加导致水凝胶的孔隙率、溶胀、载药量、药物释放和凝胶分数增加,而溶胶分数降低。因此,从结果可以得出结论,所开发的pH敏感水凝胶网络可作为靶向药物递送系统的有前景的载体。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/f77f/8951511/57736eb7fc30/gels-08-00155-g001.jpg

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