title: Novel intraocular and systemic absorption drug delivery and efficacy of N-acetylcarnosine lubricant eye drops or carcinine biologics in pharmaceutical usage and therapeutic vision care.
abstract: The latest estimates of the World Health Organization indicate that there are 161 million visually impaired individuals worldwide, 37 million of whom are blind, with a yearly increase of 1-2 million. The scientists developed and patented the lubricant eye drops formulated as 1%N-acetylcarnosine prodrug of l-carnosine containing a mucoadhesive cellulose-based compound combined with corneal absorption promoters in an ocular drug delivery system. Carcinine is suitable for the systemic administration (per oral) for ophthalmic therapeutic indications. The HPLC analysis was developed to search the pathways of ocular metabolic activities of 1%N-acetylcarnosine and the bioactivation of this drug molecule promoting transcorneal uptake of l-carnosine in the aqueous humor. A meta-analysis of phase 2 randomized double-blind placebo-controlled clinical trial data was conducted. The intraocular absorbed l-carnosine demonstrated a number of pharmacological mechanisms of prevention and reversal of cataracts. Results of systemic absorption of l-carnosine provide tuberomammillary activation that regulates neuronal functions such as hypothalamic control promoting sensory input in the primary vision perceptual pathway. The parabulbar, subconjunctival, and intravitreal injection of carcinine with most of the vehicle removed is not toxic to intraocular structures, reduces postoperative intraocular inflammation, is a potentially useful tool in the treatment of proliferative vitreoretinopathy as well as considered as the antiapoptotic drug for the protection of photoreceptor cells from oxidative light-induced stress. The discovery of naturally occurring carnosine derivatives introduces N-acetylcarnosine and carcinine as effective medical treatment for sight-threatening eye disorders.
authors.affiliation: Innovative Vision Products, Inc., County of New Castle, DE 19810, USA. markbabizhayev@mail.ru
authors.forename: Mark A
authors.initials: MA
authors.lastname: Babizhayev
authors.forename: Inna P
authors.initials: IP
authors.lastname: Khoroshilova-Maslova
authors.forename: Anne
authors.initials: A
authors.lastname: Kasus-Jacobi
mesh_terms: D060433:Administration, Ophthalmic; D000818:Animals; D002336:Carnosine / Q000008:administration & dosage / Q000031:analogs & derivatives* / Q000627:therapeutic use; D002386:Cataract / Q000188:drug therapy / Q000473:pathology; D002851:Chromatography, High Pressure Liquid / Q000379:methods; D017322:Clinical Trials, Phase II as Topic; D016503:Drug Delivery Systems; D005128:Eye Diseases / Q000188:drug therapy* / Q000473:pathology; D006801:Humans; D011355:Prodrugs; D016032:Randomized Controlled Trials as Topic; D018630:Vitreoretinopathy, Proliferative / Q000188:drug therapy / Q000473:pathology
chemical_list: D011355:Prodrugs; C033681:N-acetylcarnosine; D002336:Carnosine; C015055:carcinine