ABSTRACT

The work investigates the design and optimisation of vildagliptin (VLG)-loaded gellan gum beads for sustained release delivery. The VLG beads were prepared by the ionotropic-gelation method. A $3^2$ response surface methodology was used to optimised the effects of independent variables such as gellan gum to sodium alginate ratio ($X_1$) and concentration of CaCl₂ ($X_2$%) on dependent variables such as entrapment efficiency (EE) ($Y_1$%) and drug release (DR) ($Y_2$%). The prepared beads were characterised by employing EE, bead diameter, X-ray diffraction (XRD), Fourier transform infrared spectroscopy (FTIR), field emission scanning electron microscopy (FESEM) and DR. The values of %EE were in ranges of 76.20–91.25% and %DR was in ranges of 76.33 ± 1.64–85.12 ± 1.38% for duration of 12 hours. The optimised beads showed pH-dependent swelling and good mucoadhesivity. The VLG-loaded SA-GG beads were successfully prepared and seem to be promising for sustained release action for 12 hours duration.

摘要

这项工作研究了用于持续释放递送的维格列汀 (VLG) 负载结冷胶珠的设计和优化。VLG 珠是通过离子型凝胶法制备的。一种$3^2$ 响应面方法用于优化自变量的影响，例如结冷胶与海藻酸钠的比率（$X_1$) 和 CaCl _{2 的}浓度($X_2$%) 依赖变量，例如截留效率 (EE) (${是}_1$%) 和药物释放 (DR) (${是}_2$%）。通过使用 EE、珠直径、X 射线衍射 (XRD)、傅里叶变换红外光谱 (FTIR)、场发射扫描电子显微镜 (FESEM) 和 DR 对制备的珠进行表征。在 12 小时的持续时间内，%EE 的值在 76.20–91.25% 的范围内，%DR 的值在 76.33 ± 1.64–85.12 ± 1.38% 的范围内。优化后的珠子显示出 pH 依赖性溶胀和良好的粘膜粘附性。装载 VLG 的 SA-GG 珠子已成功制备，并且似乎有望实现 12 小时的持续释放作用。