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塞来昔布无载体可吸入干燥微粒:电喷雾技术的应用。

Carrier-Free Inhalable Dry Microparticles of Celecoxib: Use of the Electrospraying Technique.

作者信息

Jahangiri Azin, Nokhodchi Ali, Asare-Addo Kofi, Salehzadeh Erfan, Emami Shahram, Yaqoubi Shadi, Hamishehkar Hamed

机构信息

Department of Pharmaceutics, School of Pharmacy, Urmia University of Medical Sciences, Urmia 571579-9313, Iran.

Pharmaceutics Research Laboratory, School of Life Sciences, University of Sussex, Brighton BN1 9QJ, UK.

出版信息

Biomedicines. 2023 Jun 17;11(6):1747. doi: 10.3390/biomedicines11061747.

Abstract

Upregulation of cyclooxygenase (COX-2) plays an important role in lung cancer pathogenesis. Celecoxib (CLX), a selective COX-2 inhibitor, may have beneficial effects in COVID-19-induced inflammatory storms. The current study aimed to develop carrier-free inhalable CLX microparticles by electrospraying as a dry powder formulation for inhalation (DPI). CLX microparticles were prepared through an electrospraying method using a suitable solvent mixture at two different drug concentrations. The obtained powders were characterized in terms of their morphology, solid state, dissolution behavior, and aerosolization performance. Electrosprayed particles obtained from the ethanol-acetone solvent mixture with a drug concentration of 3 % / exhibited the best in vitro aerosolization properties. The value of the fine particle fraction obtained for the engineered drug particles was 12-fold higher than that of the untreated CLX. When the concentration of CLX was increased, a remarkable reduction in FPF was obtained. The smallest median mass aerodynamic diameter was obtained from the electrosprayed CLX at a 3% concentration (2.82 µm) compared to 5% (3.25 µm) and untreated CLX (4.18 µm). DSC and FTIR experiments showed no change in drug crystallinity or structure of the prepared powders during the electrospraying process. The findings of this study suggest that electrospraying has potential applications in the preparation of DPI formulations.

摘要

环氧化酶(COX - 2)的上调在肺癌发病机制中起重要作用。塞来昔布(CLX)是一种选择性COX - 2抑制剂,可能对新冠病毒诱导的炎症风暴有有益作用。本研究旨在通过电喷雾法开发无载体可吸入CLX微粒,作为干粉吸入制剂(DPI)。使用合适的溶剂混合物,通过电喷雾法在两种不同药物浓度下制备CLX微粒。对所得粉末的形态、固态、溶解行为和气雾化性能进行了表征。从药物浓度为3%的乙醇 - 丙酮溶剂混合物中获得的电喷雾颗粒表现出最佳的体外雾化性能。工程化药物颗粒的细颗粒分数值比未处理的CLX高12倍。当CLX浓度增加时,细颗粒分数显著降低。与5%(3.25 µm)和未处理的CLX(4.18 µm)相比,浓度为3%的电喷雾CLX获得的最小中位质量空气动力学直径为2.82 µm。DSC和FTIR实验表明,在电喷雾过程中,制备粉末的药物结晶度或结构没有变化。本研究结果表明,电喷雾在DPI制剂的制备中具有潜在应用。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/2948/10296448/a947db4648cb/biomedicines-11-01747-g001.jpg

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