The Journal of Supercritical Fluids ( IF 3.9 ) Pub Date : 2021-01-12 , DOI: 10.1016/j.supflu.2021.105163 Fariba Razmimanesh , Gholamhossein Sodeifian , Seyed Ali Sajadian
The present study practiced ultrasonic-assisted rapid expansion of a supercritical CO2 solution into a liquid solvent (US-RESOLV) process for the synthesis of nanoparticles (NPs) of Sunitinib malate for the first time. Hydrophilic polymers including hydroxypropyl methylcellulose (HPMC), poly (vinyl alcohol) (PVA), chitosan (CHI) and polyethylene glycol (PEG) were utilized for modifying the size distribution and increasing the dissolution rate of the Sunitinib malate NPs. Also, we determined the impact of pressure, nozzle diameter as well as temperature on morphology, size distribution and dissolution rate of produced particles. In order to accomplish the objectives of the present study, PEG was the best polymer for controlling the particle size distribution and HPMC served as the best polymeric stabilizer for increasing the dissolution rate of the drug particles. The synthesized particles were much smaller (<600 nm) in comparison to the unprocessed particles of Sunitinib malate. The combined effects of the smaller sizes of the particles, ultrasonication and the presence of polymers could enhance dissolution rate of the Sunitinib malate in the aqueous media.
中文翻译:
US-RESOLV方法研究苹果酸舒尼替尼纳米颗粒的生产:聚合物类型对溶出度和粒度分布的影响
本研究实践了超声辅助超临界CO 2的快速膨胀溶液到液体溶剂(US-RESOLV)中的过程,首次合成了苹果酸舒尼替尼的纳米颗粒(NP)。利用包括羟丙基甲基纤维素(HPMC),聚乙烯醇(PVA),壳聚糖(CHI)和聚乙二醇(PEG)在内的亲水性聚合物来改变苹果酸舒尼替尼NPs的粒径分布并提高其溶出速率。此外,我们确定了压力,喷嘴直径以及温度对所产生颗粒的形态,尺寸分布和溶解速率的影响。为了实现本研究的目的,PEG是控制颗粒大小分布的最佳聚合物,HPMC是提高药物颗粒溶解速率的最佳聚合物稳定剂。合成的颗粒小得多(< 与未处理的苹果酸舒尼替尼颗粒相比,波长为600 nm)。较小尺寸的颗粒,超声处理和聚合物的存在共同作用可以提高苹果酸舒尼替尼在水性介质中的溶解速率。