Faculty of Pharmacy & Alternative Medicine, The Islamia University of Bahawalpur, Bahawalpur, Pakistan.
Faculty of Pharmacy, University of Sargodha, Sargodha, Pakistan.
Pak J Pharm Sci. 2020 Jul;33(4):1483-1491.
The purpose of present study is to load Metformin HCl into pH-sensitive hydrogels to have sustained release over a period of time. The hydrogel was synthesized from naturally occurring polysaccharide pectin and monomer acrylic acid (AA) using ethylene glycol dimethacrylate (EGDMA) as cross-linker under controlled conditions for polymerization at 45°C for one hr, 50°C for two hrs, 55°C for three hrs, 60°C for four hrs and finally 65˚C for 12 hrs. Hydrogels were characterized for dynamic/equilibrium swelling, sol-gel fraction analysis, diffusion coefficient and percentage porosity. Hydrogels were tested by FTIR, XRD and SEM for structure and surface morphology respectively. Experimental in-vitro drug release data was applied to kinetic models. Formation of strong bonding between pectin and AA was supported by FTIR. The intensity of XRD peaks was reduced in non-loaded and loaded hydrogels compared to active drug substance. The non-loaded hydrogel showed discrete porous structure whereas loaded hydrogels were fibrous and smooth. Hydrogels showed higher swelling in the solutions of pH 6.5 and 7.5 as compared to in the solutions of pH 1.2 and 5.5. The diffusion coefficient decreases with the increase of AA and pectin concentrations. It was observed upon increasing the EGDMA concentration porosity decreases. The release of drug from all compositions of hydrogels took place through non-Fickian diffusion mechanism.
本研究的目的是将盐酸二甲双胍载入 pH 敏感水凝胶中,以在一段时间内实现持续释放。水凝胶是由天然多糖果胶和单体丙烯酸(AA)通过乙二醇二甲基丙烯酸酯(EGDMA)在受控条件下聚合合成的,聚合温度为 45°C 1 小时、50°C 2 小时、55°C 3 小时、60°C 4 小时,最后在 65°C 12 小时。对水凝胶进行了动态/平衡溶胀、溶胶-凝胶分数分析、扩散系数和孔隙率百分比的特性研究。通过傅里叶变换红外光谱(FTIR)、X 射线衍射(XRD)和扫描电子显微镜(SEM)分别对水凝胶进行了结构和表面形貌测试。对体外药物释放数据进行了动力学模型拟合。FTIR 支持果胶和 AA 之间形成了强键。与活性药物物质相比,未负载和负载水凝胶的 XRD 峰强度降低。未负载的水凝胶显示出离散的多孔结构,而负载的水凝胶则呈纤维状和光滑状。与 pH 值为 1.2 和 5.5 的溶液相比,水凝胶在 pH 值为 6.5 和 7.5 的溶液中的溶胀率更高。扩散系数随 AA 和果胶浓度的增加而降低。随着 EGDMA 浓度的增加,观察到孔隙率降低。所有水凝胶组成部分的药物释放都是通过非菲克扩散机制进行的。