Wu Hsien-Tsung, Chuang Yao-Hsiang, Lin Han-Cyuan, Chien Liang-Jung
Department of Chemical Engineering, Ming Chi University of Technology, 84 Gungjuan Rd., Taishan Dist., New Taipei City 24301, Taiwan.
Polymers (Basel). 2021 Jul 9;13(14):2260. doi: 10.3390/polym13142260.
In this study, hydroxypropyl-beta-cyclodextrin (HP-β-CD) particles were produced using supercritical assisted atomization (SAA) with carbon dioxide as the spraying medium or co-solute and aqueous ethanol solution as the solvent. The effects of several key factors on the morphology and size of the HP-β-CD particles were investigated. These factors included the solvent effect, temperatures of the precipitator and saturator, concentration of the HP-β-CD solution, and flow rate ratio of carbon dioxide to the HP-β-CD solution. The conducive conditions for producing fine spherical particles were 54.2% () aqueous ethanol as the solvent; precipitator and saturator temperatures of 373.2 K and 353.2 K, respectively; a flow rate ratio of carbon dioxide to HP-β-CD solution of 1.8; and low concentrations of HP-β-CD solution. The addition of leucine (LEU) enhanced the aerosol performance of the HP-β-CD particles, and the fine particle fraction () of the HP-β-CD particles with the addition of 13.0 mass% LEU was 1.8 times higher than that of the HP-β-CD particles without LEU. This study shows that LEU can act as a dispersion enhancer and that HP-β-CD particles produced using SAA can be used as pulmonary drug carriers.
在本研究中，以二氧化碳作为喷雾介质或共溶质，以乙醇水溶液作为溶剂，采用超临界辅助雾化（SAA）法制备了羟丙基-β-环糊精（HP-β-CD）颗粒。研究了几个关键因素对HP-β-CD颗粒形态和尺寸的影响。这些因素包括溶剂效应、沉淀器和饱和器的温度、HP-β-CD溶液的浓度以及二氧化碳与HP-β-CD溶液的流速比。制备细小球形颗粒的有利条件为：以54.2%（体积分数）的乙醇水溶液作为溶剂；沉淀器和饱和器的温度分别为373.2 K和353.2 K；二氧化碳与HP-β-CD溶液的流速比为1.8；以及低浓度的HP-β-CD溶液。亮氨酸（LEU）的添加增强了HP-β-CD颗粒的气溶胶性能，添加13.0质量%LEU的HP-β-CD颗粒的细颗粒分数（质量分数）比未添加LEU的HP-β-CD颗粒高1.8倍。本研究表明，LEU可作为分散增强剂，且采用SAA法制备的HP-β-CD颗粒可作为肺部药物载体。
