Graduate Program in Pharmaceutical Sciences, Department of Drugs and Pharmaceuticals, School of Pharmaceutical Sciences, São Paulo State University-UNESP, Rodovia Araraquara-Jaú, km 1, Zip Code 14801-902, Araraquara, SP, Brazil.
Graduate Program in Pharmaceutical Sciences, Department of Drugs and Pharmaceuticals, School of Pharmaceutical Sciences, São Paulo State University-UNESP, Rodovia Araraquara-Jaú, km 1, Zip Code 14801-902, Araraquara, SP, Brazil.
Carbohydr Polym. 2014 Nov 26;113:286-95. doi: 10.1016/j.carbpol.2014.07.021. Epub 2014 Jul 17.
Gellan gum/pectin beads were prepared by ionotropic gelation, using Al(3+) as crosslinker. High yield (92.76%) and entrapment efficiency (52.22-88.78%) were reached. Beads exhibited high circularity (0.730-0.849) and size between 728.95 and 924.56 μm. Particle size and circularity was increased by raising polymer and crosslinker concentrations. Polymers ratio did not influence beads properties. The materials stability and the absence of drug-polymers interactions were evidenced by thermal analysis and FTIR. The high beads mucoadhesiveness was evidenced by in vitro and ex vivo tests. The erosion of beads was greater in acid media while swelling was more pronounced in pH 7.4. Drug release was dependent on pH in which samples 11H1-3, 11H1-5 and 41H1-3 released only 34%, 20% and 22% of ketoprofen in pH 1.2, while in pH 7.4 the drug release was sustained up to 360 min. Korsmeyer-Peppas model demonstrated that drug release occurred according to super case-II transport.
以 Al(3+)为交联剂，采用离子凝胶法制备了结冷胶/果胶珠。产率（92.76%）和包封效率（52.22-88.78%）均较高。所得珠粒具有较高的圆度（0.730-0.849）和粒径（728.95-924.56 μm）。通过提高聚合物和交联剂的浓度可以增加粒径和圆度。聚合物比对珠粒性能没有影响。热分析和傅里叶变换红外光谱（FTIR）证明了材料的稳定性和药物-聚合物之间不存在相互作用。体外和体内试验证明了珠粒具有较高的黏膜黏附性。在酸性介质中珠粒的溶蚀性较大，而在 pH7.4 时溶胀性更为明显。药物释放取决于 pH 值，在 pH1.2 时，样品 11H1-3、11H1-5 和 41H1-3 仅释放了酮洛芬的 34%、20%和 22%，而在 pH7.4 时，药物释放可持续 360 分钟。Korsmeyer-Peppas 模型表明，药物释放符合超二级传输。
