利多卡因眼用外用溶液体外安全性评价及渗透研究

Sirikool Thamnium, V. Panapisal, J. Luckanagul
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引用次数: 0

摘要

在本研究中,我们评估了局部利多卡因溶液作为一种非侵入性麻醉药物给药的生物相容性。本研究旨在探讨药物对人角膜上皮细胞(HCECs)的细胞毒性,并评价药物的透性。在细胞毒性的情况下,用药物溶液处理HCECs,分析存活率。在渗透研究方面,采用改进的franz扩散法研究利多卡因溶液的渗透分配系数;此外,还测定了巩膜上残留的药物。采用浓度范围为0.781 ~ 100 g/L的利多卡因溶液处理HCECs。reazurin代谢率试验表明,浓度超过12 g/L时,细胞活力显著降低。由于受体腔内药物缺失,无法测定盐酸利多卡因溶液的渗透系数。全部载药留在供体腔内,并吸附在巩膜组织表面。结果表明,外用利多卡因溶液安全性较好,利多卡因滴剂不经巩膜吸收。本研究认为局部局部麻醉给药利多卡因用于眼科治疗是安全的。
本文章由计算机程序翻译,如有差异,请以英文原文为准。
In Vitro Safety Assessment and Permeation Study of Topical Lidocaine Solution for Ocular Administration
In this research, topical lidocaine solution for ocular administration was assessed for biocompatibility as a non-invasive anesthetic drug delivery. The study aimed to investigate the cytotoxicity against human corneal epithelial cells (HCECs) and to evaluate drug permeation. In the case of cytotoxicity, HCECs were treated with drug solution, analyzed for percent viability. For permeation study, the modified-franz diffusion method was used to study permeation partition coefficient of lidocaine solution; moreover, the drug retained on the sclera was also determined. HCECs were treated with lidocaine solutions with the concentration range of 0.781 -100 g/L. Significantly decrease in cell viability with the concentration above 12 g/L was detected by Resazurin metabolic rate assay. The permeation coefficient of lidocaine hydrochloride solution could not be determined because of drug absence in the receptor chamber. The entire drug loaded remained in the donor chamber and adsorbed on the surface of sclera tissue. The results suggested that topical lidocaine solution showed reasonably safe and lidocaine drops did not absorbed through the sclera. In present study, local topical anesthetic delivery of lidocaine was considered safe for ophthalmologic treatment.
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