Microemulsion: new insights into the ocular drug delivery.

ISRN Pharmaceutics Pub Date : 2013-06-27 Print Date: 2013-01-01 DOI:10.1155/2013/826798
Rahul Rama Hegde, Anurag Verma, Amitava Ghosh
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Abstract

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.

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微乳剂:眼部给药的新视角。
使用溶液等传统给药系统将药物送入眼内是治疗眼部疾病的一大挑战。泪液分泌、泪液-眼屏障和血液-眼屏障是药物从眼表流失的主要障碍。为了提高局部用药在眼部的生物利用度和延长药物在眼部的停留时间,人们制造了许多眼科给药载体。微乳剂可用作眼部给药载体,具有多种有利的制药和生物制药特性,如其出色的热力学稳定性、向液晶状态的相变、极低的表面张力和较小的液滴尺寸,可改善眼部药物滞留、延长作用时间、促进眼部吸收和药物渗透。此外,微乳剂同时具有亲脂性和亲水性的特点,因此所含药物既能被动扩散,又能在亲脂性-亲水性可变的角膜屏障中显著分区。本综述将深入探讨以往使用各种非离子表面活性剂、助表面活性剂进行眼部给药的微乳剂研究,以及这些微乳剂对眼表的潜在刺激性。所报告的体内实验表明,微乳剂中的药物具有延迟作用,并能增加药物在角膜上的渗透。
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