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Naringin processing using GAS antisolvent technique and in vivo applications
The Journal of Supercritical Fluids ( IF 3.9 ) Pub Date : 2023-12-20 , DOI: 10.1016/j.supflu.2023.106148
Patricia V. Oliveira , Jônatas L. Dias , Guilherme S.B. Sakata , Gean P.S. Aguiar , Ketelin Z. Kuhn , Otavio Sanaiotto , Ana C. Provinelli , Carla F. Daniel , Adailton Bortoluzzi , Nicola Precisvalle , Anna M. Siebel , Lindomar Alberto Lerin , Claudio Trapella , Liz G. Müller , J. Vladimir Oliveira

Naringin is a flavanone glycoside with various pharmacological activities, including neuroprotective and antipsychotic-like effects. However, it has poor solubility in water and oral bioavailability. This study aims to investigate the influence of gas antisolvent operational parameters (pressure, temperature, antisolvent flow rate, and initial concentration of solute) on particle diameter using a 24 Central Composite Design. Naringin particles produced were analyzed for dissolution rate and then applied to ketamine-induced hyperlocomotion in mice. Results for run with C= 5 mg∙mL−1, P = 12 MPa, T = 308 K, CO2 flow rate= 15 mL.min−1 showed amorphous particles while run with C= 10 mg.mL−1, P = 8 MPa, T = 318 K, CO2 flow rate= 15 mL.min−1 kept the crystalline structure of naringin. In vivo assays showed promising results for run with crystalline particles, probably due to the increased bioavailability, and amorphous particles had similar effects to commercial naringin because of the recrystallization when in contact with the aqueous medium.



中文翻译:

采用 GAS 反溶剂技术加工柚皮苷及其体内应用

柚皮苷是一种黄烷酮苷,具有多种药理活性,包括神经保护和抗精神病样作用。但其水溶性和口服生物利用度较差。本研究旨在使用 2 4中心复合设计研究气体反溶剂操作参数(压力、温度、反溶剂流速和溶质初始浓度)对粒径的影响。分析产生的柚皮苷颗粒的溶解率,然后将其应用于氯胺酮诱导的小鼠过度运动。C= 5 mg∙mL -1 , P = 12 MPa, T = 308 K, CO 2流速= 15 mL.min -1运行结果显示无定形颗粒,而 C= 10 mg.mL -1 , P运行时显示无定形颗粒= 8 MPa,T = 318 K,CO 2流量= 15 mL.min -1保持了柚皮苷的晶体结构。体内测定显示使用结晶颗粒进行的有希望的结果,可能是由于生物利用度增加,并且无定形颗粒与商业柚皮苷具有相似的效果,因为与水介质接触时会重结晶。

更新日期:2023-12-20
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