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兔角膜的体外扩散研究与莫西沙星可溶性植入物。

Ex vivo rabbit cornea diffusion studies with a soluble insert of moxifloxacin.

机构信息

Instituto de Ciencias Biomédicas, Departamento de Farmacia, Facultad de Ciencias de la Salud, Universidad Cardenal Herrera-CEU, CEU Universities, C/Santiago Ramón y Cajal, s/n., 46115, Alfara del Patriarca, Valencia, Spain.

出版信息

Drug Deliv Transl Res. 2018 Feb;8(1):132-139. doi: 10.1007/s13346-017-0443-y.

Abstract

The objective of this research was to develop and evaluate an ocular insert for the controlled drug delivery of moxifloxacin which could perhaps be used in the treatment of corneal keratitis or even bacterial endophthalmitis. We have evaluated the ex vivo ocular diffusion of moxifloxacin through rabbit cornea, both fresh and preserved under different conditions. Histological studies were also carried out. Subsequently, drug matrix inserts were prepared using bioadhesive polymers. The inserts were evaluated for their physicochemical parameters. Ophthalmic ex vivo permeation of moxifloxacin was carried out with the most promising insert. The formulate insert was thin and provided higher ocular diffusion than commercial formulations. Ocular diffusion studies revealed significant differences between fresh and frozen corneas. Histological examinations also showed differences in the thickness of stroma between fresh and frozen corneas. The ophthalmic insert we have developed allows a larger quantity of moxifloxacin to permeate through the cornea than existing commercial formulations of the drug. Ocular delivery of moxifloxacin with this insert could be a new approach for the treatment of eye diseases.

摘要

本研究旨在开发和评估一种眼部植入物,用于莫西沙星的控释给药,该植入物或许可用于治疗角膜角膜炎甚至细菌性眼内炎。我们已经评估了莫西沙星通过兔角膜的体外眼扩散,包括新鲜角膜和在不同条件下保存的角膜。还进行了组织学研究。随后,使用生物粘附聚合物制备了药物基质植入物。评估了插入物的物理化学参数。用最有前途的插入物进行了莫西沙星的眼部离体渗透实验。该配方插入物很薄,提供的眼部扩散量高于商业配方。眼部扩散研究表明,新鲜和冷冻角膜之间存在显著差异。组织学检查还显示,新鲜和冷冻角膜之间基质的厚度存在差异。我们开发的眼部植入物允许比现有商业制剂更多的莫西沙星通过角膜渗透。通过这种植入物进行莫西沙星的眼部给药可能是治疗眼部疾病的一种新方法。

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