Antioxidant properties and effects of formulation variables on Ceiba pentandra microspheres

J. O. Ayorinde, E. O. Okonye
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Abstract

Background: New drug delivery techniques have improved therapeutic and physicochemical properties of herbal medicines.Objective: Extracts of Ceiba pentandra (CP) leaf have been evaluated for antioxidant properties with the aim of formulating them into microspheres and studying release of flavonoid from the dosage form.Materials and Methods: Microspheres were prepared from extracts of CP using ionotropic gelation method. Formulation parameters were varied to produce A1 to A8. Microspheres were evaluated for size, shape, yield, micrometrics, swelling, entrapment efficiency, and flavonoid release characteristics. Factorial experimentation design was used to determine the individual and interactive effects of the formulation variables on entrapment efficiency and flavonoid release. Results were analysed using ANOVA at p≤0.05.Results: The extract contained flavonoids. Microspheres were discrete, porous, spherical, with good flow. Microspheres swelled moderately and eroded within 3 hours. Entrapment efficiencies ranged from 4.17 to 19.2 %. All Formulations released 80 % of flavonoid within 6 hours, except A2, A3 and A8 which sustained flavonoid release for 24 – 26 hours. Concentration of polymer had the highest positive effect, while stirring speed had the highest negative effect on microsphere entrapment efficiency. Effect of curing time on entrapment efficiency was positive but insignificant. Polymer concentration and curing time had negative effects on flavonoid release, while stirring speed showed a positive effect.Conclusion: Extracts of Ceiba pentandra leaves possess antioxidant constituents and could be formulated into microspheres of good physicochemical properties. Concentrations of polymer and curing time are important parameters that should be considered in the formulation of CP into microspheres with sustained release potentials.
五味子微球的抗氧化特性和配方变量的影响
背景:新的给药技术改善了中草药的治疗和理化特性:新的给药技术改善了草药的治疗和理化特性:材料与方法:采用离子凝胶法,从 Ceiba pentandra(CP)叶提取物中制备微球,并研究黄酮类化合物从该剂型中的释放情况:采用离子凝胶法从氯化石蜡提取物中制备微球。改变配方参数制备出 A1 至 A8。对微球的大小、形状、产量、微观计量学、膨胀、夹持效率和类黄酮释放特性进行了评估。采用因子实验设计来确定配方变量对夹持效率和类黄酮释放的单独和交互影响。结果采用方差分析,p≤0.05:结果:提取物中含有黄酮类化合物。微球离散、多孔、球形,流动性好。微球适度膨胀,并在 3 小时内侵蚀。包埋效率从 4.17% 到 19.2% 不等。除 A2、A3 和 A8 外,所有配方均在 6 小时内释放出 80% 的类黄酮,其中 A2、A3 和 A8 的类黄酮释放持续时间为 24 - 26 小时。聚合物的浓度对微球夹持效率的正面影响最大,而搅拌速度对微球夹持效率的负面影响最大。固化时间对夹持效率的影响为正,但不显著。聚合物浓度和固化时间对黄酮类化合物的释放有负面影响,而搅拌速度则有正面影响:结论:五味子叶提取物具有抗氧化成分,可配制成理化性质良好的微球。聚合物浓度和固化时间是将氯化石蜡配制成具有持续释放潜力的微球时应考虑的重要参数。
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