<p>A Review of the Mechanism of Action of Cyclosporine A: The Role of Cyclosporine A in Dry Eye Disease and Recent Formulation Developments</p>

Abstract

Dry eye disease (DED) is a multifactorial disease of the ocular surface and tear film that has gained awareness as a public health problem. Characteristics of DED include tear film instability, hyperosmolarity, and ocular surface inflammation, which can occur independently or may be a sequela of numerous ocular diseases, ocular surgery or contact lens wear. Much has been learned about the impact of the disease to help affected individuals who report symptoms of poor vision, pain, and tearing. Recently, new research highlights the importance of the role of ocular surface inflammation and damage in DED—leading to a vicious cycle of inflammation as well as loss of tear film homeostasis. DED immunopathophysiology is characterized by four stages: initiation, amplification, recruitment, and re-initiation. Cyclosporine is proven to be a valuable ophthalmic therapeutic for DED through its immunomodulatory actions and regulation of the adaptive immune response. Cyclosporine mechanism of action is well described in the published literature and the myriad of benefits in all four stages lend a broad-based immunomodulatory function particularly suitable for addressing DED. Furthermore, cyclosporine has unique goblet cell density improvement capabilities as well as anti-apoptotic properties. Topical formulations of cyclosporine are centered around addressing the highly lipophilic nature of the molecule. The poor aqueous solubility of cyclosporine traditionally presented technical challenges in drug delivery to the ocular surface. Newer formulations such as cationic emulsions and nanomicellar aqueous solutions address formulation, tissue concentration, and drug delivery challenges.

Mussel-Inspired Microgel Encapsulated NLRP3 Inhibitor as a Synergistic Strategy Against Dry Eye

“…Long-term or improper use of glucocorticoids can cause serious complications such as elevated intraocular pressure and cataract ( Roberti et al, 2020 ). While immunosuppressants can reduce the expression of inflammatory cytokines on the ocular surface, toxicity and side effects still limit their clinical application ( Periman et al, 2020 ). Therefore, new strategies for effective and safe treatment of DED are still urgently required.…”

A Single Administration of OC-01 (Varenicline Solution) Nasal Spray Induces Short-Term Alterations in Conjunctival Goblet Cells in Patients with Dry Eye Disease

“…Although mucin secretagogues are available in Japan for treatment of dry eye disease (e.g., the P2Y 2 receptor agonist, diquafosol, releases the mucin, MUC5AC, from conjunctival goblet cells [ 22 ]), to date, these drugs have not attained US Food and Drug Administration approval. Instead, dry eye disease is often treated with anti-inflammatory agents such as cyclosporine, which has been shown to increase the density of goblet cells over time (e.g., over 6 months of treatment), which is hypothesized to be due to anti-apoptotic activity [ 24 ], but it is unknown whether mucin secretion from goblet cells is stimulated [ 23 ]. Our goblet cell findings are similar to that observed after a single application of intranasal electrical neurostimulation [ 23 , 25 , 26 ], which also treats the signs and symptoms of dry eye disease by stimulating nerves in the nasal cavity [ 27 ].…”

Side effects of psychotropic drugs on eye

“…В запущенных случаях ССГ наблюдается снижение остроты зрения. С целью предотвращения развития данных зрительных нарушений эффективно назначение циклоспорина [12].…”