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Human biology aspects of ocular N\u2010acetylcarnosine deacetylation during its pass through the cornea to the aqueous humor and dipeptide hydrolyzing enzymes are characterized. Novel approaches to ocular drug delivery increasing intraocular bioavailability of N\u2010acetylcarnosine biologically activated metabolite carnosine become an integral development ensuring prolonged retention of the medication in the mucoadhesive precorneal area and facilitating transcorneal penetration of the natural dipeptide with the corneal promoters.<\/jats:p><jats:p>A comprehensive list of techniques for peptide drug design, synthesis, purification, and biological analyses was considered: liquid chromatography (LC), high performance liquid chromatography (HPLC), <jats:sup>1<\/jats:sup>H and <jats:sup>13<\/jats:sup>C nuclear magnetic resonance (NMR), electrospray ionization (ESI) mass spectroscopy, and spectrophotometry. The antioxidant activity of therapeutics\u2010targeted molecules was studied in aqueous solution and in a lipid membrane environment. A deglycation therapeutic system was developed involving removal, by transglycation of sugar or aldehyde moieties from Schiff bases by histidyl\u2010hydrazide compounds or aldehyde scavenger L\u2010carnosine. Clinical studies included ophthalmoscopy, visual acuity (VA), halometer disability glare tests, slit\u2010image, and retro\u2010illumination photography.<\/jats:p><jats:p>N\u2010acetylcarnosine 1% lubricant eye drops are considered as an auto\u2010induction prodrug and natural ocular redox state balance therapies with implications in prevention and treatment of serious eye diseases that involve pathways of continuous oxidative damage to ocular tissues(cataracts, primary open\u2010angle glaucoma, age\u2010related macular degeneration) and sight\u2010threatening glycosylation processes (diabetic retinopathy and consequent visual impairment) important for public health. The results of the study document that the therapeutic benefit in clinical trials is associated with the bioactivation universal antioxidant and transglycating properties of N\u2010acetylcarnosine acting as the ophthalmic prodrug of L\u2010carnosine, and depends on the nature of the specific drug delivery lubricant eye\u2010drop formulation applied as the topical solution.<\/jats:p><jats:p>The research highlights findings in N\u2010acetylcarnosine prodrug activation, transport mechanisms, drug\u2010to\u2010drug interactions, and formulations in order to unlock the optimization of complicated ocular pharmacology of N\u2010acetylcarnosine. Patented N\u2010acetylcarnosine lubricant eye\u2010drop formula was marketed as numerous human biological brands reaching important distribution networks on over 550 000 bottles sold.<\/jats:p><jats:p>Nature Does Nothing Uselessly.<\/jats:p><jats:p>\u2010Aristotle<\/jats:p><jats:p>Copyright \u00a9 2011 John Wiley &amp; Sons, Ltd.<\/jats:p>","DOI":"10.1002\/dta.265","type":"journal-article","created":{"date-parts":[[2011,3,18]],"date-time":"2011-03-18T02:13:52Z","timestamp":1300414432000},"page":"468-485","source":"Crossref","is-referenced-by-count":6,"title":["Bioactivation antioxidant and transglycating properties of N\u2010acetylcarnosine autoinduction prodrug of a dipeptide L\u2010carnosine in mucoadhesive drug delivery eye\u2010drop formulation: powerful eye health application technique and therapeutic platform"],"prefix":"10.1002","volume":"4","author":[{"given":"Mark A.","family":"Babizhayev","sequence":"first","affiliation":[],"role":[{"role":"author","vocabulary":"crossref"}]}],"member":"311","published-online":{"date-parts":[[2011,3,18]]},"reference":[{"key":"e_1_2_8_2_2","doi-asserted-by":"publisher","DOI":"10.1002\/cber.19000330275"},{"key":"e_1_2_8_3_2","doi-asserted-by":"publisher","DOI":"10.1016\/0010-406X(70)90049-6"},{"key":"e_1_2_8_4_2","doi-asserted-by":"publisher","DOI":"10.1016\/0014-2999(84)90434-5"},{"key":"e_1_2_8_5_2","doi-asserted-by":"publisher","DOI":"10.1016\/0065-2571(90)90017-V"},{"key":"e_1_2_8_6_2","doi-asserted-by":"publisher","DOI":"10.1126\/science.184.4139.909"},{"key":"e_1_2_8_7_2","first-page":"1105","article-title":"The antioxidative properties of carnosine, a natural histidine containing dipeptide","volume":"15","author":"Boldyrev A. 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