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首页> 美国卫生研究院文献>International Journal of Molecular Sciences >Optimization of Chitosan–Alginate Microparticles for Delivery of Mangostins to the Colon Area Using Box–Behnken Experimental Design
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Optimization of Chitosan–Alginate Microparticles for Delivery of Mangostins to the Colon Area Using Box–Behnken Experimental Design

机译：使用Box-Behnken实验设计优化壳聚糖-海藻酸盐微粒将芒果素递送至结肠区域的操作

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Chitosan-alginate microparticles loaded with hydrophobic mangostins present in the mangosteen rind extract have been formulated and optimized for colon-targeted bioactive drug delivery systems. The chitosan–mangostin microparticles were prepared using the ionotropic gelation method with sodium tripolyphosphate as the cross-linking agent of chitosan. The chitosan–mangostin microparticles were then encapsulated in alginate with calcium chloride as the linking agent. The mangostin release profile was optimized using the Box–Behnken design for response surface methodology with three independent variables: (A) chitosan–mangostin microparticle size, (B) alginate:chitosan mass ratio, and (C) concentration of calcium chloride. The following representative equation was obtained: percent cumulative release of mangostins (10 h) = 59.51 − 5.16A + 20.00B − 1.27C − 1.70AB − 5.43AC − 5.04BC + 0.0579A + 10.25B + 1.10C . Cumulative release of 97% was obtained under the following optimum condition for microparticle preparation: chitosan–mangosteen particle size < 100 µm, alginate:chitosan mass ratio of 0.5, and calcium chloride concentration of 4% / . The alginate to chitosan mass ratio is the statistically significant variable in the optimization of sequential release profile of mangostins in simulated gastrointestinal fluids. Furthermore, a sufficient amount of alginate is necessary to modify the chitosan microparticles and to achieve a complete release of mangostins. The results of this work indicate that the complete release of mangostins to the colon area can be achieved using the chitosan–alginate microparticles as the bioactive delivery system.
机译：载有山竹果皮提取物中存在的疏水性芒果素的壳聚糖-海藻酸盐微粒已经过配制并针对结肠靶向生物活性药物传递系统进行了优化。使用三聚磷酸钠作为壳聚糖的交联剂，采用离子凝胶法制备了壳聚糖-芒果素微粒。然后将壳聚糖-芒果素微粒包裹在藻酸盐中，用氯化钙作为连接剂。使用Box-Behnken设计针对响应表面方法优化了芒果的释放曲线，该方法具有三个独立变量：（A）壳聚糖-芒果的微粒大小，（B）海藻酸盐：壳聚糖的质量比和（C）氯化钙的浓度。获得以下代表性方程式：芒果释放的累积释放百分比（10 h）= 59.51-5.16A + 20.00B-1.27C-1.70AB-5.43AC-5.04BC + 0.0579A + 10.25B + 1.10C。在以下微粒制备的最佳条件下，累积释放量为97％：壳聚糖-山竹果粒径<100 µm，藻酸盐：壳聚糖质量比为0.5，氯化钙浓度为4％/。藻酸盐与壳聚糖的质量比是模拟胃肠液中芒果素顺序释放曲线优化中的统计学显着变量。此外，需要足够量的藻酸盐来修饰壳聚糖微粒并实现芒果素的完全释放。这项工作的结果表明，使用壳聚糖-海藻酸盐微粒作为生物活性传递系统可以实现芒果素向结肠区域的完全释放。

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