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利用体外皮肤渗透分析模型预测眼部药物渗透：姜黄素制剂的可行性研究

Utilizing an Ex Vivo Skin Penetration Analysis Model for Predicting Ocular Drug Penetration: A Feasibility Study with Curcumin Formulations.

作者信息

Raab Christian, Brugger Stefan, Lechner Jara-Sophie, Barbalho Geisa Nascimento, Gratieri Taís, Agarwal Priyanka, Rupenthal Ilva D, Keck Cornelia M

机构信息

Department of Pharmaceutics and Biopharmaceutics, Philipps-Universität Marburg, Robert-Koch-Str. 4, 35037 Marburg, Germany.

Buchanan Ocular Therapeutics Unit, Department of Ophthalmology, Aotearoa-New Zealand National Eye Centre, Faculty of Medical and Health Sciences, The University of Auckland, Auckland 1142, New Zealand.

出版信息

Pharmaceutics. 2024 Oct 6;16(10):1302. doi: 10.3390/pharmaceutics16101302.

DOI:10.3390/pharmaceutics16101302
PMID:39458631
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC11510696/
Abstract

UNLABELLED

This study aimed to investigate the feasibility of using the digital image processing technique, developed to semi-quantitatively study dermal penetration, to study corneal penetration in an ex vivo porcine eye model. Here, we investigated various formulation strategies intended to enhance dermal and corneal bioavailability of the model hydrophobic drug, curcumin.

METHODS

Several formulation principles were explored, including oily solutions, oily suspensions, aqueous nanosuspension, micelles, liposomes and cyclodextrins. The dermal penetration efficacy was tested using an ex vivo porcine ear model previously developed at Philipps-Universität Marburg with subsequent digital image processing. This image analysis method was further applied to study corneal penetration using an ex vivo porcine whole-eye model.

RESULTS

For dermal penetration, oily solutions, oily suspensions and nanosuspensions exhibited the least penetration, whereas liposomes and cyclodextrins showed enhanced penetration. Corneal curcumin penetration correlated with dermal penetration, with curcumin loaded into cyclodextrins penetrating the deepest.

CONCLUSIONS

Overall, our study suggests that the image analysis method previously developed for ex vivo skin penetration can easily be repurposed to study corneal penetration of hydrophobic drugs.

摘要

未标注

本研究旨在探讨利用为半定量研究皮肤渗透而开发的数字图像处理技术，在离体猪眼模型中研究角膜渗透的可行性。在此，我们研究了旨在提高模型疏水药物姜黄素的皮肤和角膜生物利用度的各种制剂策略。

方法

探索了几种制剂原理，包括油溶液、油混悬液、水性纳米混悬液、胶束、脂质体和环糊精。使用先前由马尔堡菲利普斯大学开发的离体猪耳模型，通过后续的数字图像处理来测试皮肤渗透效果。这种图像分析方法进一步应用于使用离体猪全眼模型研究角膜渗透。

结果

对于皮肤渗透，油溶液、油混悬液和纳米混悬液的渗透最少，而脂质体和环糊精显示出增强的渗透。角膜姜黄素渗透与皮肤渗透相关，负载到环糊精中的姜黄素渗透最深。

结论

总体而言，我们的研究表明，先前为离体皮肤渗透开发的图像分析方法可以轻松地重新用于研究疏水药物的角膜渗透。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/f4f8/11510696/c3a21d18c47c/pharmaceutics-16-01302-g011.jpg
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https://cdn.ncbi.nlm.nih.gov/pmc/blobs/f4f8/11510696/4a202f4a9083/pharmaceutics-16-01302-g006.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/f4f8/11510696/424b0a56b390/pharmaceutics-16-01302-g007.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/f4f8/11510696/a3074127f20e/pharmaceutics-16-01302-g008.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/f4f8/11510696/081886db103a/pharmaceutics-16-01302-g009.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/f4f8/11510696/f5d4375b33e0/pharmaceutics-16-01302-g010.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/f4f8/11510696/c3a21d18c47c/pharmaceutics-16-01302-g011.jpg

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