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基于西多福韦自溶 Soluplus 的聚合物薄膜:一种改善眼部感染管理的新方法。

Ciprofloxacin self-dissolvable Soluplus based polymeric films: a novel proposal to improve the management of eye infections.

机构信息

Department of Pharmacy and Pharmaceutical Technology and Parasitology, University of Valencia, Avda. Vicente A. Estelles SN, Burjassot Valencia, Spain.

Department of Microbiology and Ecology, University of Valencia, Avda. Vicente A. Estelles SN, Burjassot Valencia, Spain.

出版信息

Drug Deliv Transl Res. 2021 Apr;11(2):608-625. doi: 10.1007/s13346-020-00887-1. Epub 2021 Feb 2.

Abstract

Infections of the eye are among the leading causes of vision impairment and vision loss worldwide. The ability of a drug to access the anterior parts of the eye is negligible after systemic administration. Effective drug delivery to the eye is a major challenge due to the presence of protective mechanisms and physiological barriers that result in low ocular availability after topical application. The main purpose of this work was the improvement of the corneal and conjunctival permeation of the antibiotic Ciprofloxacin, a wide spectrum antibiotic used for the most common eye infection, using a self-dissolving polymeric film. Films were prepared by the solvent casting technique, using polyvinyl caprolactam-polyvinyl acetate-polyethylene glycol graft co-polymer (Soluplus), polyvynyl alcohol, and propylene glycol. Films were homogeneous in drug content and thickness, as demonstrated by adapting the Swiss Roll technique followed by microscopy observation. These films proved in vitro to control the release of the Ciprofloxacin. Ex vivo permeability studies using Franz diffusion cells and porcine cornea and sclera showed an effective permeability of the drug without inducing irritation of the tissues. Films swelled in contact with artificial tears forming an in situ gel over 20 min, which will improve drug contact and reduce the need of multiple dosing. The antibiotic activity was also tested in vitro in five types of bacterial cultures, assuring the pharmacological efficacy of the films. The developed films are a promising drug delivery system to topically treat or prevent ocular infections.

摘要

眼部感染是全球导致视力损害和视力丧失的主要原因之一。全身给药后,药物到达眼部前部的能力可以忽略不计。由于存在保护机制和生理屏障,药物经局部应用后眼部可用性较低,因此有效递送至眼部是一个主要挑战。这项工作的主要目的是使用自溶解聚合物膜来改善抗生素环丙沙星的角膜和结膜渗透。使用聚乙烯己内酰胺-聚醋酸乙烯酯-聚乙二醇接枝共聚物(Soluplus)、聚乙烯醇和丙二醇通过溶剂浇铸技术制备了薄膜。通过适应瑞士卷技术并进行显微镜观察,证明这些薄膜在药物含量和厚度方面具有均一性。这些薄膜在体外证明可以控制环丙沙星的释放。使用 Franz 扩散细胞和猪角膜和巩膜进行的体外渗透研究表明,药物具有有效的渗透性,而不会引起组织刺激。薄膜与人工泪液接触后会在 20 分钟内膨胀形成原位凝胶,这将改善药物接触并减少多次给药的需求。还在五种类型的细菌培养物中对薄膜的抗生素活性进行了体外测试,确保了薄膜的药理功效。开发的薄膜是一种有前途的局部递药系统,可用于治疗或预防眼部感染。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/ea9b/7852484/23c6835ed287/13346_2020_887_Fig1_HTML.jpg

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