氯雷他定负载热响应水凝胶:表征和离体兔角膜渗透性研究

Behzad Sharif Makhmalzadeh, A. Salimi, Aida Niroomand
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引用次数: 3

摘要

滴眼液的生物利用度差主要是由于滴眼液通过鼻泪管引流,通过角膜上皮的渗透性很低。我们研究的目的是制备和表征氯雷他定眼水凝胶,作为亲脂性药物的一个例子,以增加药物浓度和在眼睛作用部位的停留时间。在本研究中,采用23全因子设计来设计和比较8种不同氯雷他定水凝胶配方的性能。结果表明,水凝胶的溶胀率和孔隙率与配方中的Pluronic百分比和Pluronic/carbomer比具有显著的相关性。此外,所有制剂的释放曲线均显示出快速和持续的释放。通过FT-IR技术对水凝胶结构的评价表明,Pluronic与卡波姆中的羟基和羧基相互作用,这是形成水凝胶网络的主要原因,并与氯雷他定相互作用。氯雷他定通过兔角膜的渗透性实验表明,F2和F7剂型的药物渗透率分别是对照组的15倍和70倍。
本文章由计算机程序翻译,如有差异,请以英文原文为准。
Loratadine-Loaded Thermoresponsive Hydrogel: Characterization and Ex-vivo Rabbit Cornea Permeability Studies
Poor bioavailability of ophthalmic drops is mainly due to drainage through the nasal-lacrimal duct and a very low permeability through corneal epithelium. The aim of our study was to prepare and characterize an ocular hydrogel of loratadine, as an example of a lipophilic drug, to increase drug concentration and residence time at the site of action in the eye. In this study, a 23 full factorial design was employed to design and compare the properties of eight different loratadine containing hydrogel formulations. Results showed a significant correlation between the swelling and porosity ratios of the hydrogels and the Pluronic percentage and Pluronic/carbomer ratio in the formulations. Moreover, the release profiles showed fast and sustained release of all the formulations. Evaluation of hydrogels structure by the FT-IR technique indicated that Pluronic interacts with hydroxyl and carboxylic groups in carbomer, which is the main reason of the hydrogel network formation and interacts with loratadine.The permeation of loratadine through rabbit cornea showed that drug permeation percentages for the F2 and F7 formulations were 15 and 70 folds more than that of the control.
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