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首页> 外文期刊>Journal of Microencapsulation: Microcapsules Liposomes Nanoparticles Microcells Microspheres >Optimizing formulation factors in preparing chitosan microparticles by spray-drying method
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Optimizing formulation factors in preparing chitosan microparticles by spray-drying method

机译:喷雾干燥法制备壳聚糖微粒的配方优化

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The chitosan only, chitosan/Pluronic F68, chitosan/gelatin, chitosan/Pluronic F68/gelatin microparticles and betamethasone-loaded chitosan/Pluronic F68/gelatin microparticles were successfully prepared by a spray-drying method. Microparticle characteristics (yield rate, zeta potential, particle size and tap density), loading efficiencies, microparticle morphology and in-vitro release properties were investigated. By properly choosing excipient type, concentration and varying the spray-drying parameters, a high degree of control was achieved over the physical properties of the dry chitosan powders. SEM micrograph shows that the particle sizes of the varied chitosan composed microparticles ranged from 2.12-5.67 mum and the external surfaces appear smooth. Using betamethasone as model drug, the spray-drying is a promising way to produce good spherical and smooth surface microparticles with a narrow particle size range for controlled delivery of betamethasone. The positively charged betamethasone-loaded microparticles entrapped in the chitosan/Pluronic F68/gelatin microparticles with trapping efficiencies up to 94.5%, yield rate 42.5% and mean particle size 5.64 mum varied between 4.32-6.20 mum and tap densities 0.128 g/cm~3. The pH of particle was increased with increasing betamethasone-loaded amount, but both zeta potential and tap density of the particles decreased with increasing betamethasone-loaded amount. The betamethasone release rates from chitosan/Pluronic F68/gelatin microparticles were influenced by the drug/polymer ratio in the manner that an increase in the release% and burst release% was observed when the drug loading was decreased. The in vitro release of betamethasone showed a dose-dependent burst followed by a slower release phase that was proportional to the drug concentration in the concentration range between 14-44% w/w.
机译:通过喷雾干燥法成功地制备了仅壳聚糖,壳聚糖/ Pluronic F68,壳聚糖/明胶,壳聚糖/ Pluronic F68 /明胶微粒和载有倍他米松的壳聚糖/ Pluronic F68 /明胶微粒。研究了微粒特征(屈服速率,ζ电位,粒径和振实密度),负载效率,微粒形态和体外释放特性。通过适当选择赋形剂类型,浓度和改变喷雾干燥参数,可以高度控制壳聚糖干粉的物理性能。 SEM显微照片显示,各种壳聚糖组成的微粒的粒径范围为2.12-5.67μm,并且其外表面显得光滑。使用倍他米松作为模型药物,喷雾干燥是一种生产具有良好粒径和窄粒径范围的球形和光滑表面微粒的良好方法,可控制倍他米松的递送。截留在壳聚糖/ Pluronic F68 /明胶微粒中的带正电荷的倍他米松微粒的捕集效率高达94.5%,产率42.5%,平均粒径5.64微米,介于4.32-6.20微米之间,振实密度为0.128 g / cm〜3。 。颗粒的pH值随倍他米松负载量的增加而增加,但粒子的zeta电位和振实密度随倍他米松负载量的增加而降低。壳聚糖/ Pluronic F68 /明胶微粒的倍他米松释放速率受药物/聚合物比率的影响,其方式为:当减少载药量时,观察到释放%增加和爆发释放%。倍他米松的体外释放显示出剂量依赖性的爆发,随后是一个缓慢的释放阶段,该阶段与浓度在14-44%w / w之间的药物浓度成比例。

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