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抗坏血酸脂质体配方对角膜通透性的影响。

Effect of liposomal formulation of ascorbic acid on corneal permeability.

机构信息

Department of Ophthalmology, Semmelweis University, Mária Street 39., 1085, Budapest, Hungary.

Institute of Pharmaceutical Technology and Regulatory Affairs, Faculty of Pharmacy, University of Szeged, Eötvös Street 6., 6720, Szeged, Hungary.

出版信息

Sci Rep. 2023 Mar 1;13(1):3448. doi: 10.1038/s41598-023-29290-9.

DOI:10.1038/s41598-023-29290-9
PMID:36859418
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC9977777/
Abstract

Ascorbic acid (AA) has a pivotal role in corneal wound healing via stimulating the biosynthesis of highly organized extracellular matrix components, but its rapid degradation and low corneal permeability limits its therapeutic effects. In this paper, we present the pharmacokinetic properties of a liposomal-based formulation of AA in terms of corneal permeation. Chemical stability, shelf-life, and drug release rate of lyophilized liposome (AA-LLipo) formulation was determined in comparison to free-form of AA solution using high-performance liquid chromatography (HPLC) and rapid equilibrium dialysis. In vitro transcorneal permeability was studied using a parallel artificial membrane permeability assay (PAMPA). Ex vivo permeation was examined on AA-LLipo-treated porcine cornea by determining the AA content on the ocular surface, in the cornea as well as in the aqueous humor using HPLC, and by Raman-mapping visualizing the AA-distribution. Our results showed that the liposomal formulation improved the chemical stability of AA, while drug release was observed with the same kinetic efficiency as from the free-form of AA solution. Both corneal-PAMPA and porcine corneal permeability studies showed that AA-LLipo markedly improved the corneal absorption kinetics of AA, thus, increasing the AA content in the cornea and aqueous humor. AA-LLipo formulation could potentially increase the bioavailability of AA in corneal tissues.

摘要

抗坏血酸（AA）通过刺激高度组织化细胞外基质成分的生物合成，在角膜伤口愈合中起着关键作用，但它的快速降解和低角膜通透性限制了其治疗效果。在本文中，我们介绍了基于脂质体的 AA 制剂在角膜渗透方面的药代动力学特性。使用高效液相色谱法（HPLC）和快速平衡透析法，与游离 AA 溶液相比，我们确定了冻干脂质体（AA-LLipo）制剂的化学稳定性、保质期和药物释放率。使用平行人工膜渗透测定法（PAMPA）研究了体外跨角膜渗透性。通过 HPLC 测定眼表、角膜和房水中的 AA 含量，以及通过拉曼映射可视化 AA 分布，研究了 AA-LLipo 处理的猪角膜的离体渗透情况。我们的结果表明，脂质体制剂提高了 AA 的化学稳定性，而药物释放与游离 AA 溶液的动力学效率相同。角膜 PAMPA 和猪角膜通透性研究均表明，AA-LLipo 显著改善了 AA 的角膜吸收动力学，从而增加了角膜和房水中的 AA 含量。AA-LLipo 制剂有可能增加 AA 在角膜组织中的生物利用度。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/109e/9977777/ac2847286dc3/41598_2023_29290_Fig7_HTML.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/109e/9977777/0e1313b26cf5/41598_2023_29290_Fig1_HTML.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/109e/9977777/58409c08927d/41598_2023_29290_Fig2_HTML.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/109e/9977777/4af888a87e9f/41598_2023_29290_Fig3_HTML.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/109e/9977777/d4e3cff5bda4/41598_2023_29290_Fig4_HTML.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/109e/9977777/eb0ff0cb2213/41598_2023_29290_Fig5_HTML.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/109e/9977777/6a259351e66b/41598_2023_29290_Fig6_HTML.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/109e/9977777/ac2847286dc3/41598_2023_29290_Fig7_HTML.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/109e/9977777/0e1313b26cf5/41598_2023_29290_Fig1_HTML.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/109e/9977777/58409c08927d/41598_2023_29290_Fig2_HTML.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/109e/9977777/4af888a87e9f/41598_2023_29290_Fig3_HTML.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/109e/9977777/d4e3cff5bda4/41598_2023_29290_Fig4_HTML.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/109e/9977777/eb0ff0cb2213/41598_2023_29290_Fig5_HTML.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/109e/9977777/6a259351e66b/41598_2023_29290_Fig6_HTML.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/109e/9977777/ac2847286dc3/41598_2023_29290_Fig7_HTML.jpg

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