The role of topical N-acetylcysteine in ocular therapeutics

• Published in: Survey of ophthalmology Vol. 67; no. 2; pp. 608 - 622
• Main Authors: Eghtedari, Yas, Oh, Lawrence J., Girolamo, Nick Di, Watson, Stephanie L.
• Format: Journal Article
• Language: English
• Published: United States Elsevier Inc 01.03.2022
• Subjects: Acetylcysteine - administration & dosage; Acetylcysteine - chemistry; Administration, Topical; Antioxidant; Chitosan; Cornea; Cornea - drug effects; Dry eye; Dry Eye Syndromes - drug therapy; Humans; N-acetylcysteine; Ocular burns; Topical therapeutics; Cornea; Ocular burns; Antioxidant; Dry eye; Topical therapeutics; N-acetylcysteine
• ISSN: 0039-6257; 1879-3304
• DOI: 10.1016/j.survophthal.2021.07.008

N-acetylcysteine (NAC) was first discovered as a mucolytic agent in 1960. We investigate the role of topical NAC in ocular therapeutics, including its mechanism of action, current applications, and adverse effects. A systematic search of peer-reviewed articles identified 106 references including in vitro, in vivo and clinical studies on the use of NAC in the treatment of ocular diseases. NAC can be synthetically manufactured, and its mechanisms of action include mucolysis, scavenging hydroxyl radicals, and modulation of inflammatory cascades. These unique properties contribute to the diverse applications of NAC, including its steroid-sparing potential. NAC has been used topically in the treatment of corneal wounds, chemical injuries, keratitis, dry eye disease and meibomian gland dysfunction. The clinical benefits of NAC are evident over a wide range of concentrations, the most common being 5-10% topical NAC applied four times daily. Adverse effects such as corneal necrosis are rare, but have been reported with higher doses. NAC also has potential applications in laser epithelial keratomileusis, diabetic eye disease, retinitis pigmentosa, senile nuclear cataracts, macular degeneration, and cigarette smoke-induced corneal damage. Recently, chitosan-NAC has been used as a nanocarrier for the topical administration of medications to the ocular surface. Owing to its potent antioxidant, anti-inflammatory and mucolytic properties, topical NAC has had extensive use in the treatment of ocular pathology.