Hegde Rahul Rama, Verma Anurag, Ghosh Amitava
School of Pharmaceutical Sciences, IFTM University, Lodhipur Rajput, Moradabad 244102, India.
ISRN Pharm. 2013 Jun 27;2013:826798. doi: 10.1155/2013/826798. Print 2013.
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.
使用传统给药系统(如溶液)将药物递送至眼部,对眼部疾病的治疗是一项重大挑战。泪液分泌、泪液-眼屏障和血-眼屏障导致药物从眼表流失,这些是主要障碍。人们已研发出多种眼科给药载体,以提高生物利用度并延长局部应用于眼部的药物的停留时间。微乳作为一种眼部给药载体的潜在用途具有若干良好的药学和生物药学特性,例如其出色的热力学稳定性、向液晶态的相转变、极低的表面张力以及小液滴尺寸,这可能会改善药物在眼部的滞留、延长作用持续时间、提高眼部吸收以及所载药物的渗透。此外,微乳兼具亲脂性和亲水性特征,使得所载药物既能被动扩散,又能在可变的亲脂-亲水角膜屏障中显著分配。本综述将深入探讨此前关于使用各种非离子表面活性剂、助表面活性剂的微乳用于眼部给药的研究,以及其对眼表的相关刺激可能性。已报道的体内实验表明,微乳中所含药物具有延迟效应,且药物的角膜渗透率有所增加。