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用气凝胶进行肺部药物输送:藻酸盐和藻酸盐-透明质酸微球的工程设计。

Pulmonary drug delivery with aerogels: engineering of alginate and alginate-hyaluronic acid microspheres.

机构信息

Institute of Thermal Separation Processes, Hamburg University of Technology, Hamburg, Germany.

Institute of Pharmacy, Division of Pharmaceutical Technology, University of Hamburg, Hamburg, Germany.

出版信息

Pharm Dev Technol. 2021 Jun;26(5):509-521. doi: 10.1080/10837450.2021.1888979. Epub 2021 Mar 19.

DOI:10.1080/10837450.2021.1888979
PMID:33593203
Abstract

In this study, the aerogel technology was used to prepare pulmonary drug carriers consisting of alginate and alginate-hyaluronic acid by an emulsion gelation technique and supercritical CO drying. During the preparation process, the emulsification rate and inner phase viscosity were varied to control the diameter of aerogel microspheres. Results showed that the aerogel microspheres were highly porous (porosity > 98%) with low densities in the range between 0.0087 and 0.0634 g/cm as well as high surface areas between 354 and 759 m/g. The obtained microspheres showed aerodynamic diameter below 5 µm making them suitable for pulmonary drug delivery. An drug release study with the model drug sodium naproxen was conducted and a non-Fickian drug release mechanism was observed, with no significant difference between the release profiles of alginate and alginate-hyaluronic acid microspheres. During the emulsion gelation step, the feasibility of using the capillary number to estimate the largest stable droplet size in the emulsions was also studied and it was found that using this number, the droplet size in the emulsions may well be predicted.

摘要

在这项研究中,采用气凝胶技术通过乳化凝胶技术和超临界 CO2 干燥法制备由海藻酸钠和海藻酸钠-透明质酸组成的肺部药物载体。在制备过程中,通过改变乳化速率和内相粘度来控制气凝胶微球的直径。结果表明,气凝胶微球具有高孔隙率(>98%)、低密度(在 0.0087 到 0.0634 g/cm3 之间)和高比表面积(354 到 759 m2/g)。所得微球的空气动力学直径低于 5 μm,适合肺部药物输送。对模型药物萘普生钠进行了药物释放研究,观察到非菲克扩散药物释放机制,海藻酸钠和海藻酸钠-透明质酸微球的释放曲线没有显著差异。在乳化凝胶步骤中,还研究了使用毛细数估计乳液中最大稳定液滴尺寸的可行性,结果发现使用该数,可以很好地预测乳液中的液滴尺寸。

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