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用于肺部给药的高性能姜黄素纳米晶体的体外和体内评价

Evaluation of High-Performance Curcumin Nanocrystals for Pulmonary Drug Delivery Both In Vitro and In Vivo.

作者信息

Hu Liandong, Kong Dongqian, Hu Qiaofeng, Gao Na, Pang Saixi

机构信息

School of Pharmaceutical Sciences, Hebei University, No. 180, WuSi Road, Baoding, 071002, People's Republic of China.

Key Laboratory of Pharmaceutical Quality Control of Hebei Province, Hebei University, Baoding, People's Republic of China.

出版信息

Nanoscale Res Lett. 2015 Dec;10(1):381. doi: 10.1186/s11671-015-1085-y. Epub 2015 Oct 1.

Abstract

This paper focused on formulating high-performance curcumin spray-dried powders for inhalation (curcumin-DPIs) to achieve a high lung concentration. Curcumin-DPIs were produced using wet milling combined with the spray drying method. The effects of different milling times on particle size and aerodynamic performance were investigated. The curcumin-DPIs were characterized by scanning electron microscopy (SEM), differential scanning calorimetry (DSC), powder X-ray diffraction (PXRD), Fourier transform infrared spectroscopy (FTIR), and in vitro dissolution. Furthermore, the in vivo pharmacokinetic behavior and tissue distribution after pulmonary administration were also evaluated. Results showed that the drug dissolution was significantly enhanced by processing into curcumin-DPIs. The aerodynamic results indicated that the DPIs displayed a good aerosol performance. The plasma curcumin concentration was obviously enhanced by inhalation, and most of the curcumin-DPIs were deposited in the lung. This study demonstrated that inhalation was an effective way to carry drug to the lung, and curcumin-DPIs were hopeful for lung cancer treatment in the future.

摘要

本文着重于制备用于吸入的高性能姜黄素喷雾干燥粉末(姜黄素干粉吸入剂)以实现肺部高浓度。姜黄素干粉吸入剂采用湿磨结合喷雾干燥法制备。研究了不同研磨时间对粒径和空气动力学性能的影响。通过扫描电子显微镜(SEM)、差示扫描量热法(DSC)、粉末X射线衍射(PXRD)、傅里叶变换红外光谱(FTIR)和体外溶出度对姜黄素干粉吸入剂进行了表征。此外,还评估了肺部给药后的体内药代动力学行为和组织分布。结果表明,制成姜黄素干粉吸入剂后药物溶出显著增强。空气动力学结果表明,干粉吸入剂表现出良好的气溶胶性能。吸入明显提高了血浆姜黄素浓度,且大部分姜黄素干粉吸入剂沉积在肺部。本研究表明,吸入是将药物输送到肺部的有效途径,姜黄素干粉吸入剂有望在未来用于肺癌治疗。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/1063/4591223/a3a3939570fc/11671_2015_1085_Fig2_HTML.jpg

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