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Preparation and characterization of flurbiprofen-loaded poly(3-hydroxybutyrate-co-3-hydroxyvalerate) microspheres

机译:负载氟比洛芬的聚(3-羟基丁酸酯-co-3-羟基戊酸酯)微球的制备与表征

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Poly(3-hydroxybutyrate-co-3-hydroxyvalerate) (PHBV) microspheres containing flurbiprofen were prepared by an oil-in-water emulsion solvent evaporation method,in order to develop a particulate drug delivery system for localized administration.A response surface method (RSM) using a central composite design was employed to evaluate the effect of the poly(vinyl alcohol) (PVA) (%,w/v) concentration in the aqueous phase and the PHBV concentration in the organic phase (%,w/v) on some of the resulting microspheres properties.The response variables were the encapsulation efficiency (EE),the mean particle size,the width of particle size distribution (expressed by the SPAN value) and the required time for the in vitro release of 50% of the encapsulated drug (t_(50%)).Second-order polynomial and linear equations were fitted to experimental data and were also used to interpret the results.Results indicated that the concentration of the stabilizer (PVA) showed a highly negative effect on the EE probably due to the increased drug solubility in the aqueous phase as a result of the higher PVA concentrations.Particle diameter mean size increased with the increased polymer concentration while the width of the particle size distribution was found to decrease with the increase of the stabilizer agent.Finally,results indicated that none of the investigated variables presented a significant effect on the t_(50%) values.
机译:通过水包油乳液溶剂蒸发法制备了含有氟比洛芬的聚3-羟基丁酸酯-3-羟基戊酸酯共聚物(PHBV)微球,以开发用于局部给药的颗粒药物递送系统。使用中央复合设计的RSM)评估了水相中聚乙烯醇(PVA)(%,w / v)浓度和有机相中PHBV浓度(%,w / v)的影响响应变量包括包封效率(EE),平均粒径,粒径分布宽度(用SPAN值表示)和50%的体外释放所需的时间。实验数据拟合了二阶多项式和线性方程,并用来解释结果。结果表明,稳定剂(PVA)的浓度对药物具有很高的负面影响。 EE专业版可能是由于较高的PVA浓度导致药物在水相中的溶解度增加。颗粒直径的平均尺寸随聚合物浓度的增加而增加,而粒径分布的宽度随稳定剂的增加而减小。最后,结果表明,所研究的变量均未对t_(50%)值产生显着影响。

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