Srinivasan Sruthi, Williams Ravaughn
Alcon Research LLC, Johns Creek, GA, 30097, USA.
Clin Ophthalmol. 2022 Oct 10;16:3311-3326. doi: 10.2147/OPTH.S377960. eCollection 2022.
Dry eye disease (DED) is a chronic condition of the ocular surface characterized by a loss of the tear film homeostasis and accompanied by symptoms such as eye discomfort and visual disturbances. DED is classified as aqueous deficient dry eye (ADDE), evaporative dry eye (EDE), and mixed dry eye etiologies. The mainstay treatment in the management of DED is artificial tear drops or lubricant eye drops that replenish the aqueous and/or lipid layer of the tear film. These are available as both lipid-based and non-lipid-based formulations, with/without preservatives. Lipid-based lubricant eye drops can stabilize the tear film lipid layer, reduce tear evaporation, and improve signs of EDE. In this review, we present the formulation components, mechanism of action, and summary of preclinical and clinical evidence on a lipid-based formulation - propylene glycol-hydroxypropyl guar (PG-HPG) nanoemulsion lubricant eye drops (Systane Complete). These eye drops consist of the demulcent (lubricant), PG (0.6%). HPG forms a soft, thin, cross-linked in situ gel matrix with borate ions, when exposed to the tear film, which prolongs lubricant retention and provides ocular surface protection. Dimyristoyl phosphatidyl glycerol, an anionic phospholipid, helps in replenishing the lipid layer of the tear film. Moreover, the nanoemulsion formulation serves as a depot for delivery of dimyristoyl phosphatidyl glycerol to enhance ocular surface coverage. Preclinical and clinical evidence demonstrate that PG-HPG nanoemulsion lubricant eye drops are safe and effective in providing temporary relief of symptoms of DED, regardless of its subtypes. Specifically, it provides sustained reduction in dry eye symptoms, improves tear film stability/lipid layer grade, and improves ocular surface characteristics.
干眼症(DED)是一种眼表慢性疾病,其特征是泪膜稳态失衡,并伴有眼不适和视觉障碍等症状。DED分为水液缺乏型干眼症(ADDE)、蒸发过强型干眼症(EDE)和混合型干眼症病因。DED治疗的主要方法是使用人工泪液或润滑滴眼液来补充泪膜的水液层和/或脂质层。这些滴眼液有基于脂质和非脂质的配方,有/无防腐剂。基于脂质的润滑滴眼液可以稳定泪膜脂质层,减少泪液蒸发,并改善EDE的症状。在本综述中,我们介绍了一种基于脂质的配方——丙二醇-羟丙基瓜尔胶(PG-HPG)纳米乳剂润滑滴眼液(思然全效)的配方成分、作用机制以及临床前和临床证据总结。这些滴眼液由保湿剂(润滑剂)、PG(0.6%)组成。HPG在接触泪膜时与硼酸根离子形成柔软、薄的原位交联凝胶基质,从而延长润滑剂的保留时间并提供眼表保护。二肉豆蔻酰磷脂酰甘油是一种阴离子磷脂,有助于补充泪膜的脂质层。此外,纳米乳剂配方可作为二肉豆蔻酰磷脂酰甘油的递送载体,以增强眼表覆盖。临床前和临床证据表明,PG-HPG纳米乳剂润滑滴眼液在缓解DED症状方面是安全有效的,无论其亚型如何。具体而言,它能持续减轻干眼症状,改善泪膜稳定性/脂质层等级,并改善眼表特征。