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采用简化的级联冲击器法对同时载有厄洛替尼和金雀异黄素的雾化脂质体的气溶胶特性进行研究。

Aerosol characterisation of nebulised liposomes co-loaded with erlotinib and genistein using an abbreviated cascade impactor method.

机构信息

UCL School of Pharmacy, 29-39 Brunswick Square, London WC1N 1AX, United Kingdom.

UCL School of Pharmacy, 29-39 Brunswick Square, London WC1N 1AX, United Kingdom.

出版信息

Int J Pharm. 2018 May 5;542(1-2):8-17. doi: 10.1016/j.ijpharm.2018.02.035. Epub 2018 Feb 26.

Abstract

Erlotinib and genistein co-loaded liposomes were prepared by the thin-film hydration method. The effect of probe sonication as a size reduction method on drug incorporation and the properties of aerosols generated using air-jet and vibrating-mesh nebulisers was studied. The use of the Next Generation Impactor (NGI) to characterise inhaler formulations is limited by the need accurately to quantify drug deposited across 8 stages and is labour intensive to use. The Fast Screening Impactor (FSI) comprising two impaction stages was compared with the NGI to evaluate its applicability as a simple screening and labour-saving tool to characterise nebulised systems. For the developed liposomal formulations, an air-jet nebuliser generated a two-fold higher fine particle fraction (FPF) than a vibrating-mesh nebuliser. The findings demonstrated that the cooled FSI (5°C) operated at 15 L/min was effective in differentiating the aerosol properties of the nebulised liposome formulations investigated. Overall, the optimised co-loaded liposomes were more effectively delivered by an air-jet nebuliser, than from a vibrating-mesh nebuliser over a 10 min period as determined using the abbreviated impactor.

摘要

厄洛替尼和染料木黄酮共载脂质体采用薄膜水化法制备。研究了探针超声作为一种减小粒径的方法对药物包封的影响,以及空气射流和振动网雾化器产生的气溶胶的性质。下一代撞击器(NGI)用于描述吸入器制剂的应用受到需要准确地量化跨越 8 个阶段沉积的药物的限制,并且使用起来劳动强度大。由两个撞击阶段组成的快速筛选撞击器(FSI)与 NGI 进行了比较,以评估其作为一种简单的筛选和节省劳动力的工具来描述雾化系统的适用性。对于开发的脂质体配方,空气射流雾化器产生的细颗粒分数(FPF)比振动网雾化器高两倍。研究结果表明,在 15 L/min 的冷却 FSI(5°C)下运行时,可有效区分所研究的雾化脂质体配方的气溶胶性质。总体而言,与使用缩短的撞击器在 10 分钟内相比,空气射流雾化器更有效地输送了优化的共载脂质体。

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