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黄原胶和海藻酸盐基质作为吡罗昔康和酮康唑的透皮给药载体。

Xanthan and alginate-matrix used as transdermal delivery carrier for piroxicam and ketoconazole.

机构信息

"Petru Poni" Institute of Macromolecular Chemistry, Grigore Ghica Voda Alley 41A, Iasi 70048, Romania.

"Petru Poni" Institute of Macromolecular Chemistry, Grigore Ghica Voda Alley 41A, Iasi 70048, Romania.

出版信息

Int J Biol Macromol. 2022 Jun 1;209(Pt B):2084-2096. doi: 10.1016/j.ijbiomac.2022.04.189. Epub 2022 Apr 29.

DOI:10.1016/j.ijbiomac.2022.04.189
PMID:35500769
Abstract

This study presents new drug delivery systems based on xanthan, unmodified or modified by esterification with oleic acid, and alginate for controlled release of bioactive substances with anti-inflammatory (piroxicam) and antifungal properties (ketoconazole). The mechanical properties of the developed drug carriers showed that their compressive strength was affected by the encapsulation of the bioactive principles. When ketoconazole was added into the xanthan/alginate matrix, an increment in the mechanical strength was recorded (66.68% compression). The release of the active principles from the materials was best described by the Korsmeyer-Peppas model, with non-Fickian or Fickian diffusion (the values of the exponent of release are between 0.29 and 0.75), depending on the composition of the polymeric matrix. The release rate constant presents smaller values for the materials based on chemically modified xanthan (between 0.89 and 20.11) as compared with materials based on the unmodified form (between 4.27 and 25.00). All materials were characterized by Fourier Transform Infrared Spectroscopy (FTIR) and Scanning Electron Microscopy (SEM). The designed systems prove to have antimicrobial and anti-inflammatory activity. The findings make prone these biomaterials for the manufacture of transdermal drug delivery systems.

摘要

本研究提出了基于黄原胶的新型药物传递系统,黄原胶未经修饰或用油酸酯化修饰,并与海藻酸钠结合用于控制释放具有抗炎(吡罗昔康)和抗真菌特性(酮康唑)的生物活性物质。所开发的药物载体的机械性能表明,它们的压缩强度受到封装生物活性原理的影响。当酮康唑被加入到黄原胶/海藻酸钠基质中时,记录到机械强度的增加(压缩 66.68%)。活性物质从材料中的释放最好用 Korsmeyer-Peppas 模型来描述,具有非 Fickian 或 Fickian 扩散(释放指数的值在 0.29 和 0.75 之间),这取决于聚合基质的组成。与基于未修饰形式的材料(4.27 至 25.00 之间)相比,基于化学修饰的黄原胶的材料的释放速率常数具有较小的值(0.89 至 20.11 之间)。所有材料均通过傅里叶变换红外光谱(FTIR)和扫描电子显微镜(SEM)进行了表征。设计的系统被证明具有抗菌和抗炎活性。这些发现使这些生物材料适合制造透皮药物传递系统。

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