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采用超临界气体抗溶剂(GAS)法制备盐酸帕唑帕尼纳米颗粒(抗肾癌药物)。

Production of pazopanib hydrochloride nanoparticles (anti-kidney cancer drug) using a supercritical gas antisolvent (GAS) method.

作者信息

Bazaei Majid, Honarvar Bizhan, Esfandiari Nadia, Sajadian Seyed Ali, Aboosadi Zahra Arab

机构信息

Department of Chemical Engineering, Marvdasht Branch, Islamic Azad University Marvdasht Iran

Department of Chemical Engineering, Faculty of Engineering, University of Kashan Kashan 87317-53153 Iran.

出版信息

RSC Adv. 2024 Dec 18;14(54):39844-39857. doi: 10.1039/d4ra07079h. eCollection 2024 Dec 17.

Abstract

Supercritical fluid-based methods have been receiving increasing popularity in the production of pharmaceutical nanoparticles due to their ability to control the size and distribution of the particles and offer high purity products. The gas anti-solvent method is one of the methods in which a supercritical fluid serves as an anti-solvent. The aim of this work is to develop pazopanib hydrochloride nanoparticles as an anti-cancer agent by the supercritical GAS method. For this purpose, nanoparticles were produced at different temperatures (313, 323 and 333 K), pressures (10, 13 and 16 MPa), and initial solute concentrations (12, 22 and 32 mg ml) employing the Box-Behnken design. The results showed that pressure had the most significant effect on the particle size. The average initial particle size of unprocessed pazopanib hydrochloride was about 37.5 ± 8.7 μm. The optimum process parameter values were determined to obtain the smallest particle size using the BBD method. The parameters were optimized at 320 K, 16 MPa, and 12.6 mg ml. The average particle size was 311.1 nm, close to the predicted value of 302.3 nm. FTIR analysis indicated that the chemical structure remained unaltered. Furthermore, DSC and XRD results confirmed the reduction in particle size.

摘要

基于超临界流体的方法在药物纳米颗粒生产中越来越受欢迎,因为它们能够控制颗粒的大小和分布,并提供高纯度产品。气体抗溶剂法是超临界流体用作抗溶剂的方法之一。本研究的目的是通过超临界气体抗溶剂法制备盐酸帕唑帕尼纳米颗粒作为抗癌剂。为此,采用Box-Behnken设计在不同温度(313、323和333K)、压力(10、13和16MPa)以及初始溶质浓度(12、22和32mg/ml)下制备纳米颗粒。结果表明,压力对粒径影响最为显著。未处理的盐酸帕唑帕尼的平均初始粒径约为37.5±8.7μm。使用BBD方法确定了获得最小粒径的最佳工艺参数值。这些参数在320K、16MPa和12.6mg/ml下进行了优化。平均粒径为311.1nm,接近预测值302.3nm。FTIR分析表明化学结构未发生改变。此外,DSC和XRD结果证实了粒径的减小。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/ab03/11653517/feb08713c188/d4ra07079h-f1.jpg

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