J Pharm Pharmacol. 2014 Apr;66(4):531-41. doi: 10.1111/jphp.12075.
OBJECTIVES: Topical ocular administration is the most convenient route of administration of drugs for the treatment of eye diseases. However, the bioavailability of drugs following eye instillations of eye drops is very low. Over the past 20 years, extensive efforts have been put into research to improve drug bioavailability without compromising treatment compliance and patients' quality of life. KEY FINDINGS: One of the most efficient ways to improve drug bioavailability is to increase the precorneal residence time of the eye drop formulations. As a result, new eye drops, with bioadhesive properties, have been developed based on the cationic oil-in-water (o/w) nanoemulsion technology. These low viscosity eye drop nanoemulsions have improved precorneal residence time through the electrostatic interactions between the positively charged oil nanodroplets and the negatively charged ocular surface epithelium. SUMMARY: This review is the first to present the benefits of this new strategy used to improve ocular drug bioavailability. The roles of the cationic agent in the stabilization of a safe cationic o/w nanoemulsion have been discussed, as well as the unexpected benefits of the cationic o/w nanoemulsion for the protection and restoration of a healthy tear film and corneal epithelium.
目的:眼部局部给药是治疗眼部疾病的最方便的药物给药途径。然而,滴眼剂滴入眼睛后药物的生物利用度非常低。在过去的 20 年中,人们进行了广泛的研究,试图在不影响治疗顺应性和患者生活质量的情况下提高药物的生物利用度。
主要发现:提高药物生物利用度最有效的方法之一是增加滴眼剂配方在眼前部的停留时间。因此,基于阳离子油包水(o/w)纳米乳液技术,开发了具有生物黏附特性的新型滴眼剂。这些低粘度的滴眼纳米乳液通过带正电荷的油纳米液滴与带负电荷的眼表面上皮之间的静电相互作用,提高了在眼前部的停留时间。
总结:这是第一篇介绍这种用于提高眼部药物生物利用度的新策略的益处的综述。本文讨论了阳离子剂在稳定安全的阳离子 o/w 纳米乳液中的作用,以及阳离子 o/w 纳米乳液在保护和恢复健康的泪膜和角膜上皮方面的意外益处。
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