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首页> 外文期刊>International Journal of Pharmaceutical Investigation >Mesalamine-loaded mucoadhesive microsphere for colon drug delivery system: Effect of process variables and in vitro characterization
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Mesalamine-loaded mucoadhesive microsphere for colon drug delivery system: Effect of process variables and in vitro characterization

机译：装载美沙拉敏的粘膜粘附微球用于结肠给药系统：过程变量和体外表征的影响

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Objective: The main objective of this study is to formulate mucoadhesive microspheres for colon drug delivery with sodium alginate (ALG) core enriched with drug. Methods: The core microspheres of ALG were prepared by modified emulsification method followed by cross-linking with different concentration of CaCl2at different stirring speed with constant drug-to-polymer ratio (1:3). The core microspheres were further coated with Eudragit S-100 using the solvent evaporation technique. Results: The microspheres (core and coated) were characterized by shape, size, surface morphology, size distribution, entrapment efficiency, and in vitro drug release studies. In vitro drug release showed that the optimized batch of core microsphere and coated microspheres exhibited 99.53% ± 0.39% and 89.22% ± 0.26%, respectively. The drug release from all formulations of mesalamine microsphere followed Higuchian Kinetics. Moreover, drug release from core and Eudragit S-100-coated microspheres followed Korsmeyer–Peppas equation with anomalous and Fickian kinetics mechanism, respectively. Stability study suggests that the degradation rate constant of mesalamine from Eudragit S-100-coated microsphere was found to be minimum 2 years shelf life of the formulation. On the basis of scanning electron microscopy, the core microspheres were formed slightly irregular in shape due to surface-attached crystals of the drug and coated mesalamine microspheres showed smooth surface and a smaller number of pores due to coating. Conclusions: It can be concluded that the appropriate combination of a pH-dependent polymer (Eudragit S-100) with a pH-independent polymer sodium ALG) was suitably adequately sustained the drug release from mesalamine microspheres.
机译：目的：本研究的主要目的是用富含药物的海藻酸钠（ALG）核心配制用于结肠给药的粘膜粘附微球。方法：采用改进的乳化法制备ALG核心微球，然后以不同的搅拌速度和恒定的药物-聚合物比（1：3）与不同浓度的CaCl 2 交联。使用溶剂蒸发技术将核心微球进一步涂覆Eudragit S-100。结果：通过形状，大小，表面形态，大小分布，包封效率和体外药物释放研究对微球（核和包衣）进行了表征。体外药物释放表明，最优化批次的核心微球和包衣微球分别表现出99.53％±0.39％和89.22％±0.26％。美沙拉敏微球的所有制剂的药物释放均遵循Higuchian动力学。此外，药物从核心和Eudragit S-100包被的微球中的释放分别遵循具有异常和Fickian动力学机理的Korsmeyer-Peppas方程。稳定性研究表明，发现从Eudragit S-100涂层微球中的美沙拉敏的降解速率常数至少为该制剂的2年保质期。在扫描电子显微镜的基础上，由于药物的表面附着的晶体，核心微球的形状略微不规则，而涂覆的美沙拉敏微球由于涂覆而显示出光滑的表面和较少数量的孔。结论：可以得出结论，pH依赖性聚合物（Eudragit S-100）与pH无关聚合物钠（ALG）的适当组合可适当地充分维持美沙拉敏微球的药物释放。

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