Tsai Fu-Hsuan, Kitamura Yutaka, Kokawa Mito
Graduate School of Life and Environmental Sciences, University of Tsukuba, 1-1-1 Tennodai, Tsukuba, Ibaraki 305-8577, Japan.
Faculty of Life and Environmental Sciences, University of Tsukuba, 1-1-1 Tennodai, Tsukuba, Ibaraki 305-8577, Japan.
Int J Biol Macromol. 2017 Mar;96:600-610. doi: 10.1016/j.ijbiomac.2016.12.056. Epub 2016 Dec 23.
Liquid-core hydrogel beads (LHB) were formulated through reverse spherification, by sodium alginate and using calcium lactate (CL) to replace the common calcium source, calcium chloride. The effect of four independent variables: first gelation time (X), CL concentration in first gelation (X), secondary gelation time (X), and CL concentration in secondary gelation (X), on seven physical properties of LHB: diameter, hardness (Y), loading efficiency (LE, Y), release amount of total phenolic compounds (TP) in simulated gastric (Y) and small intestinal (Y) fluid, swelling capacity (Y), and sphericity (Y), were evaluated. Furthermore, a central composite design with response surface methodology was used for the optimization of LHB properties Y-Y, and the importance of the four independent variables to physical properties was analyzed. The diameter of LHB was in the range of 4.17-5.84mm. The optimal conditions of LHB formulation were first gelation time of 23.99min, 0.13M CL in the first gelation, secondary gelation time of 6.04min, and 0.058M CL in secondary gelation. The optimized formulation of LHB demonstrated 25.5N of hardness, 85.67% of LE and 27.38% of TP release in simulated gastric fluid with the small error-values (-2.47 to 2.21%).
液芯水凝胶珠(LHB)通过反向球化法制备,以海藻酸钠为原料,使用乳酸钙(CL)替代常用的钙源氯化钙。研究了四个自变量:初次凝胶化时间(X₁)、初次凝胶化时CL的浓度(X₂)、二次凝胶化时间(X₃)和二次凝胶化时CL的浓度(X₄)对LHB七种物理性质的影响,这七种物理性质分别为:直径、硬度(Y₁)、负载效率(LE,Y₂)、在模拟胃液(Y₃)和小肠液(Y₄)中总酚类化合物(TP)的释放量、溶胀能力(Y₅)和球形度(Y₆)。此外,采用响应面法的中心复合设计对LHB的Y₁ - Y₆性质进行优化,并分析了四个自变量对物理性质的重要性。LHB的直径范围为4.17 - 5.84毫米。LHB制剂的最佳条件为初次凝胶化时间23.99分钟、初次凝胶化时CL浓度为0.13M、二次凝胶化时间6.04分钟、二次凝胶化时CL浓度为0.058M。优化后的LHB制剂在模拟胃液中的硬度为25.5N,负载效率为85.67%,TP释放率为27.38%,误差值较小(-2.47至2.21%)。