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在压力定量吸入器中由合成表面活性剂Synsurf介导的利奈唑胺的沉积与输送：Calu-3模型

Deposition and transport of linezolid mediated by a synthetic surfactant Synsurf within a pressurized metered dose inhaler: a Calu-3 model.

作者信息

van Rensburg Lyné, van Zyl Johann M, Smith Johan

机构信息

Division of Clinical Pharmacology, Department of Medicine, Faculty of Medicine and Health Sciences, Stellenbosch University, Tygerberg, South Africa.

Department of Pediatrics, Tygerberg Children's Hospital, Faculty of Medicine and Health Sciences, Stellenbosch University, Tygerberg, South Africa.

出版信息

Drug Des Devel Ther. 2018 May 4;12:1107-1118. doi: 10.2147/DDDT.S147035. eCollection 2018.

DOI:10.2147/DDDT.S147035
PMID:29765201
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC5942168/
Abstract

BACKGROUND

Previous studies in our laboratory demonstrated that a synthetic peptide containing lung surfactant enhances the permeability of chemical compounds through bronchial epithelium. The purpose of this study was to test two formulations of Synsurf combined with linezolid as respirable compounds using a pressurized metered dose inhaler (pMDI).

METHODS

Aerosolization efficiency of the surfactant-drug microparticles onto Calu-3 monolayers as an air interface culture was analyzed using a Next Generation Impactor™.

RESULTS

The delivered particles and drug dose showed a high dependency from the preparation that was aerosolized. Scanning electron microscopy imaging allowed for visualization of the deposited particles, establishing them as liposomal-type structures (diameter 500 nm to 2 μm) with filamentous features.

CONCLUSION

The different surfactant drug combinations allow for an evaluation of the significance of the experimental model system, as well as assessment of the formulations providing a possible noninvasive, site-specific, delivery model via pMDI.

摘要

背景

我们实验室之前的研究表明，一种含肺表面活性剂的合成肽可增强化合物透过支气管上皮的通透性。本研究的目的是使用压力定量吸入器（pMDI）测试两种与利奈唑胺联合作为可吸入化合物的Synsurf制剂。

方法

使用下一代撞击器™分析表面活性剂-药物微粒在作为空气界面培养的Calu-3单层细胞上的雾化效率。

结果

递送的颗粒和药物剂量高度依赖于雾化的制剂。扫描电子显微镜成像使沉积颗粒可视化，确定它们为具有丝状特征的脂质体类型结构（直径500纳米至2微米）。

结论

不同的表面活性剂-药物组合有助于评估实验模型系统的意义，以及评估通过pMDI提供可能的非侵入性、位点特异性递送模型的制剂。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/987c/5942168/293c912d731f/dddt-12-1107Fig11.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/987c/5942168/38680ab01ba8/dddt-12-1107Fig1.jpg
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https://cdn.ncbi.nlm.nih.gov/pmc/blobs/987c/5942168/f36ffdca9367/dddt-12-1107Fig4.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/987c/5942168/27eda82428da/dddt-12-1107Fig5.jpg
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https://cdn.ncbi.nlm.nih.gov/pmc/blobs/987c/5942168/9f3746ca7f45/dddt-12-1107Fig7.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/987c/5942168/c31ad1e0fdf7/dddt-12-1107Fig8.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/987c/5942168/91cb4e1b1984/dddt-12-1107Fig9.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/987c/5942168/817965eaab1d/dddt-12-1107Fig10.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/987c/5942168/293c912d731f/dddt-12-1107Fig11.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/987c/5942168/38680ab01ba8/dddt-12-1107Fig1.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/987c/5942168/f45d8bb3d8f2/dddt-12-1107Fig2.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/987c/5942168/6f8923a8a909/dddt-12-1107Fig3.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/987c/5942168/f36ffdca9367/dddt-12-1107Fig4.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/987c/5942168/27eda82428da/dddt-12-1107Fig5.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/987c/5942168/f107762896f0/dddt-12-1107Fig6.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/987c/5942168/9f3746ca7f45/dddt-12-1107Fig7.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/987c/5942168/c31ad1e0fdf7/dddt-12-1107Fig8.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/987c/5942168/91cb4e1b1984/dddt-12-1107Fig9.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/987c/5942168/817965eaab1d/dddt-12-1107Fig10.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/987c/5942168/293c912d731f/dddt-12-1107Fig11.jpg

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