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Microemulsion: New Insights into the Ocular Drug Delivery

机译:微乳剂:眼用药物输送的新见解

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摘要

Delivery of drugs into eyes using conventional drug delivery systems, such as solutions, is a considerable challenge to the treatment of ocular diseases. Drug loss from the ocular surface by lachrymal fluid secretion, lachrymal fluid-eye barriers, and blood-ocular barriers are main obstacles. A number of ophthalmic drug delivery carriers have been made to improve the bioavailability and to prolong the residence time of drugs applied topically onto the eye. The potential use of microemulsions as an ocular drug delivery carrier offers several favorable pharmaceutical and biopharmaceutical properties such as their excellent thermodynamic stability, phase transition to liquid-crystal state, very low surface tension, and small droplet size, which may result in improved ocular drug retention, extended duration of action, high ocular absorption, and permeation of loaded drugs. Further, both lipophilic and hydrophilic characteristics are present in microemulsions, so that the loaded drugs can diffuse passively as well get significantly partitioned in the variable lipophilic-hydrophilic corneal barrier. This review will provide an insight into previous studies on microemulsions for ocular delivery of drugs using various nonionic surfactants, cosurfactants, and associated irritation potential on the ocular surface. The reported in vivo experiments have shown a delayed effect of drug incorporated in microemulsion and an increase in the corneal permeation of the drug.
机译:使用诸如溶液的常规药物输送系统将药物输送到眼睛中对于眼病的治疗是相当大的挑战。主要的障碍是泪液分泌,泪液眼屏障和血眼屏障引起的眼表药物流失。已经制备了许多眼科药物递送载体以改善生物利用度并延长局部施用到眼睛上的药物的停留时间。微乳剂作为眼用​​药物输送载体的潜在用途可提供多种有利的药物和生物药物性能,例如其优异的热力学稳定性,向液晶状态的相变,非常低的表面张力和小的液滴尺寸,这可能会改善眼用药物滞留,延长作用时间,高眼吸收和负载药物渗透。此外,微乳液中同时存在亲脂性和亲水性特征,因此负载的药物可以被动地扩散,并且在可变的亲脂性亲水性角膜屏障中显着分配。这篇综述将提供对以前使用各种非离子表面活性剂,助表面活性剂以及在眼表面的相关刺激潜力进行眼部给药的微乳剂研究的真知灼见。所报道的体内实验表明,微乳中掺入的药物具有延迟作用,并且药物的角膜渗透性增加。

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