Abbas Ali Khidher, Alhamdany Anas Tarik
Mustansiriyah University, College of Pharmacy, Department of Pharmaceutics, Baghdad, Iraq.
Turk J Pharm Sci. 2020 Apr;17(2):159-171. doi: 10.4274/tjps.galenos.2018.15046. Epub 2020 Apr 24.
The purpose of this study was to provide a control drug delivery system through a newly approved work to enhance the absorption and bioavailability of enalapril maleate loaded floating microspheres by ionotropic gelation technique using a hydrophilic carrier.
Eleven developed formulations of floating microspheres were prepared by ionotropic gelation using different concentrations of sodium alginate, iota-carrageenan, sodium bicarbonate, calcium chloride, and the drug. These microspheres were characterized using a diversity of parameters like micrometric properties, percentage yield, entrapment efficiency, buoyancy, drug release, and kinetics of drug release. The optimum formula was evaluated and identified for drug-excipients compatibility using fourier transform-infrared spectroscopy (FT-IR), surface morphology, powder X-ray diffraction (XRD), and differential scanning calorimetry (DSC).
From the results, F4 was selected as the optimum formula since it provides a faster and premium release of drug from the matrix (91.4%). Kinetics of drug release was found to depend on both diffusion and erosion mechanisms, as the correlation coefficient (R2) was best fitted with Korsmeyer's model and the release exponent (n) was shown to be between 0.43 and 0.84. Scanning electron microscopy images demonstrated spherical, discrete, and freely flowing microspheres with a particle size of 199.4±0.04 μm. Optimum buoyancy properties, percentage yield, and drug entrapment efficiency were achieved. FT-IR showed no interaction between enalapril and the polymers. DSC and XRD showed the miscibility of the drug with the polymers while maintaining the stable crystalline properties of enalapril loaded in the prepared microspheres.
The developed floating microspheres of enalapril maleate can be considered a promising controlled drug delivery system, thereby improving patient compliance.
本研究的目的是通过一项新批准的工作提供一种控释药物递送系统，以利用亲水性载体通过离子凝胶法提高马来酸依那普利载药漂浮微球的吸收和生物利用度。
采用不同浓度的海藻酸钠、角叉菜胶、碳酸氢钠、氯化钙和药物，通过离子凝胶法制备了11种漂浮微球制剂。这些微球通过多种参数进行表征，如微观特性、产率百分比、包封率、浮力、药物释放和药物释放动力学。使用傅里叶变换红外光谱（FT-IR）、表面形态、粉末X射线衍射（XRD）和差示扫描量热法（DSC）对最佳配方进行评估并确定药物-辅料相容性。
结果表明，F4被选为最佳配方，因为它能使药物从基质中更快、更优质地释放（91.4%）。药物释放动力学发现取决于扩散和侵蚀机制，因为相关系数（R2）与Korsmeyer模型拟合最佳，释放指数（n）显示在0.43至0.84之间。扫描电子显微镜图像显示微球呈球形、离散且自由流动，粒径为199.4±0.04μm。实现了最佳的浮力特性、产率百分比和药物包封率。FT-IR显示依那普利与聚合物之间没有相互作用。DSC和XRD显示药物与聚合物可混溶，同时保持制备的微球中载有的马来酸依那普利的稳定结晶性质。
所开发的马来酸依那普利漂浮微球可被认为是一种有前景的控释药物递送系统，从而提高患者的依从性。
