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聚二甲基硅氧烷透皮贴剂中孔隙结构实现药物控释

Controlled Drug Release by the Pore Structure in Polydimethylsiloxane Transdermal Patches.

作者信息

Mikolaszek Barbara, Kazlauske Jurgita, Larsson Anette, Sznitowska Malgorzata

机构信息

Department of Pharmaceutical Technology, Faculty of Pharmacy, Medical University of Gdansk, Hallera 107 Street, 80-210 Gdansk, Poland.

Pharmaceutical Technology, Department of Chemistry and Chemical Engineering, Chalmers University of Technology, SE-412 96 Gothenburg, Sweden.

出版信息

Polymers (Basel). 2020 Jul 8;12(7):1520. doi: 10.3390/polym12071520.

DOI:10.3390/polym12071520
PMID:32650625
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC7407597/
Abstract

The use of polydimethylsiloxanes (PDMS) as a drug carrier in transdermal adhesive patches is limited and there is insufficient data on the polymer structure and diffusivity, especially when additives modify the matrix. PDMS films with liquid additives (10% /): silicone oil (SO), polyoxyethylene glycol (PEG) or propylene glycol (PG) were prepared and indomethacin (IND; 5% /) was incorporated as a model active substance. The microstructure of the PDMS matrix and its permeability to water was investigated and correlated to the kinetics of the in-vitro IND release from the film. Three microscopic techniques were used to characterize in detail the microstructure of PDMS films: scanning electron microscopy, fluorescent microscopy and atomic force microscopy. PDMS films with hydrophilic PEG or PG showed different two-phase structures. A two-fold increase in steady-state flux of IND and increased water transport in the presence of PEG was attributed to the pore-like channels created by this polar solvent in the PDMS matrix. This effect was not observed in the films with PG, where only discontinuous droplet-like structures were visible. All additives significantly changed the tensile parameters of the films but the effects were not very pronounced.

摘要

聚二甲基硅氧烷(PDMS)在透皮贴剂中作为药物载体的应用有限,关于聚合物结构和扩散率的数据不足,尤其是当添加剂改变基质时。制备了含有液体添加剂(10% /)的PDMS膜:硅油(SO)、聚氧乙烯二醇(PEG)或丙二醇(PG),并掺入吲哚美辛(IND;5% /)作为模型活性物质。研究了PDMS基质的微观结构及其对水的渗透性,并将其与膜中IND的体外释放动力学相关联。使用三种显微镜技术详细表征了PDMS膜的微观结构:扫描电子显微镜、荧光显微镜和原子力显微镜。含有亲水性PEG或PG的PDMS膜呈现出不同的两相结构。在PEG存在下,IND的稳态通量增加了两倍,并且水传输增加,这归因于这种极性溶剂在PDMS基质中形成的孔状通道。在含有PG的膜中未观察到这种效应,在该膜中仅可见不连续的液滴状结构。所有添加剂均显著改变了膜的拉伸参数,但影响不太明显。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/3b2f/7407597/8c3258d8aa2e/polymers-12-01520-g007.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/3b2f/7407597/7015e8eaacab/polymers-12-01520-g001.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/3b2f/7407597/b3925cb96843/polymers-12-01520-g002.jpg
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https://cdn.ncbi.nlm.nih.gov/pmc/blobs/3b2f/7407597/c1dd256690eb/polymers-12-01520-g004.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/3b2f/7407597/02cfe0eacaad/polymers-12-01520-g005.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/3b2f/7407597/b4749d7b91d4/polymers-12-01520-g006.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/3b2f/7407597/8c3258d8aa2e/polymers-12-01520-g007.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/3b2f/7407597/7015e8eaacab/polymers-12-01520-g001.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/3b2f/7407597/b3925cb96843/polymers-12-01520-g002.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/3b2f/7407597/ec35245ff3f6/polymers-12-01520-g003.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/3b2f/7407597/c1dd256690eb/polymers-12-01520-g004.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/3b2f/7407597/02cfe0eacaad/polymers-12-01520-g005.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/3b2f/7407597/b4749d7b91d4/polymers-12-01520-g006.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/3b2f/7407597/8c3258d8aa2e/polymers-12-01520-g007.jpg

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