A considerable interest in
N-acetylcarnosine ocular
drug design for eye health is based on clinical strategies to improve ocular
drug delivery through metabolic enzymatic activation. Human biology aspects of ocular
N-acetylcarnosine 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-acetylcarnosine 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. A comprehensive list of techniques for
peptide drug design, synthesis, purification, and
biological analyses was considered: liquid chromatography (LC), high performance liquid chromatography (HPLC), (1) H and (13) C nuclear magnetic resonance (NMR), electrospray ionization (ESI) mass spectroscopy, and spectrophotometry. The
antioxidant activity of
therapeutics-targeted 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-
hydrazide compounds or
aldehyde scavenger
L-carnosine. Clinical studies included ophthalmoscopy, visual acuity (VA), halometer disability glare tests, slit-image, and retro-illumination photography.
N-acetylcarnosine 1%
lubricant eye drops are considered as an auto-induction
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-angle glaucoma,
age-related macular degeneration) and sight-threatening 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-acetylcarnosine acting as the ophthalmic
prodrug of
L-carnosine, and depends on the nature of the specific
drug delivery
lubricant eye-drop formulation applied as the topical
solution. The research highlights findings in
N-acetylcarnosine prodrug activation, transport mechanisms,
drug-to-drug interactions, and formulations in order to unlock the optimization of complicated ocular pharmacology of
N-acetylcarnosine. Patented
N-acetylcarnosine lubricant eye-drop formula was marketed as numerous human
biological brands reaching important distribution networks on over 550 000 bottles sold. Nature Does Nothing Uselessly. -Aristotle