The basic idea in this study relates to the interesting research problem to employ with the knowledgeable pharmacy staff
N-acetylcarnosine (NAC) in the developed suitable compounded
prodrug ophthalmic preparations, which are currently used for the treatment of
cataract and have
antioxidant effect, in order to provide the molecular support to one of the most popular beliefs of the growing market for the treatment of senile
cataract in patients and animals with efficacious NAC
drug formulations worldwide patented by the author. This work presents the progress in ocular NAC
prodrug and codrug design and delivery in light of revealed ocular metabolic activities. There is a considerable interest in the ophthalmic codrug design including NAC
prodrug based on the strategies to improve ophthalmic
drug delivery of the active
peptide principal
L-carnosine through the sustained intraocular metabolic activation of a
dipeptide while making it resistant to enzymatic hydrolysis. Novel approaches to ocular NAC
drug delivery, developed by Innovative Vision Products, Inc. (IVP), aim at enhancing the
drug bioavailability by ensuring a prolonged retention of the medication in the eye, and/or by facilitating transcorneal penetration. IVP team studied the effects of
lubricant eye drops designed as 1% NAC
prodrug of
L-carnosine containing a mucoadhesive
cellulose-based and corneal absorption promoters in a drug delivery system. The predicted responses of the corneal and conjunctival penetrations to the synergistic promoters are useful in controlling the extent and pathway of the ocular and systemic absorptions of instilled NAC
prodrug in designed ophthalmic formulations thereof. Utility of
peptidase enzyme inhibitors in the codrug formulation to modulate the transport and metabolism of NAC
prodrug appears to be a promising strategy for enhancing
dipeptide drug transport across the cornea. The developed and officially CE mark registered by IVP NAC
prodrug and codrug
lubricating eye drop systems (including principal regulatory registered
eye drops design and
lubricating eye drops marketed under numerous brand labels), increase the intraocular uptake of the active principle
L-carnosine from its ophthalmic carrier NAC in the aqueous humor and the permeability of a
drug into the eye, and so enhance the ocular bioavailability, bioactivating universal
antioxidant, and anti-
cataract efficacy (in human and in canine eyes) of the developed NAC
eye drops.