Pilocarpine eye drops (Vuity)

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VUITY™ may help elderly people to read without their reading glasses [1]

Elderly people can soon read without the help of their reading glasses, thanks to a just recently FDA-approved eye drop, named VUITY™ by Alergan, an AbbVie company. The product could replace reading glasses for all those who have trouble seeing close up after age 40-50, their estimated number just in US is 128 millions. This innovative ophthalmic product, described as an eye drop can be “life changer”.

How does VUITY work? The active ingredient of VUITY is pilocarpine hydrochloride. The ophthalmic solution contains 1.25 % of pilocarpine hydrochloride, a cholinergic muscarinic receptor agonist, prepared as an isotonic, colorless, sterile ophthalmic solution. Each mL of VUITY contains pilocarpine hydrochloride 12.5 mg as the active ingredient, equivalent to 1.06% (10.6 mg) pilocarpine free-base. The preservative is benzalkonium chloride 0.0075%. Inactive ingredients in the VUITY ophthalmic solution are: boric acid, sodium citrate dihydrate, sodium chloride, purified water, and may also include hydrochloric acid and/or sodium hydroxide for pH adjustment to between 3.5 and 5.5, if necessary. Pilocarpine hydrochloride contracts certain muscles in the eye to help elderly see up close.

Indication: VUITY is indicated for the treatment of presbyopia in adults.

Presbyopia: Presbyopia is physiological insufficiency of eye accommodation associated with the aging of the eye that results in progressively worsening ability to focus clearly on close objects. This is also referred to as „reading blur” affecting many adults over the age of 40. The symptoms include difficulty reading small print which results in having to hold reading material farther away. In a presbyopic eye, the clear lens gets gradually harder and harder, and does not change shape as easily, which makes it difficult to focus on near objects. In a non-presbyopic eye, the clear lens behind the iris can easily change its shape and focuses light to the retina, making it easier to see things up close.

Results of clinical studies: In clinical studies where patients received one drop of VUITY in each eye once daily, its healing potency was measured by the proportion of patients achieving a 3-line gain or more reading a near vision eye chart without losing more than 1 line in a distance vision eye chart at Day 30, 3 hours after dosing.

Cyclodextrins and pilocarpine interaction

The interaction between cyclodextrins and pilocarpine has long been studied and the consequences of cyclodextrin complexation are also well known. About 520 papers and numerosu patents are dedicated to the cyclodextrin-enabled pilocarpine formulations. The application of CDs, mainly aims at the improvement of aqueous solubility, corneal permeation, absorption and stability of the drug. [3] A number of seminal papers wer published by Department Pharmaceutical Chemistry, University Kuopio, in Finland. Finnish studies focused on the utility of HPBCD and SBECD (Captisol) for improving efficacy of pilocarpine ophthalmic compositions. [4-6]

Some publications deal with the separation of pilocarpine isomers using cyclodextrins, such as the J. Chromatography paper where cis-trans isomers of pilocarpine were well separated by CD-assisted capillary electrophoresis. [7]

References

[1] https://people.com/health/fda-approved-eye-drug-vuity-improves-close-up-vision/

[2] Khurana, AK “Asthenopia, anomalies of accommodation and convergence”. Theory and practice of optics and refraction (2nd edition). Elsevier. pp.100–107. September 2008.

[3] Freedman KA; Klein JW; Crosson CE Beta-cyclodextrins enhance bioavailability of pilocarpine.Curr Eye Res 1993 Jul;12(7):641-7 1994. (HPBCDI)

[4] (Ref: Jarho, P. et al. Hydroxypropyl-.beta.-cyclodextrin increases the aqueous solubility and stability of pilocarpine prodrugs Pharm. Res. (1995), 12(9), 1371-5, 1995

[5] Jarvinen,T;et al. Sulfobutyl ether beta-cyclodextrin SBE-beta-CD) in eyedrops improves the tolerability of a topically applied pilocarpine prodrug in rabbits J-Ocul-Pharmacol-Ther. 1995 Summer; 11(2): 95-106

[6] Jarho, P. et al Modified b-cyclodextrin (SBE7-beta-CD) with viscous vehicle improves the ocular delivery and tolerability of pilocarpine prodrug in rabbits J. Pharm. Pharmacol. (1996), 48(3), 263-269

[7] Peterson, T.Separation of drug stereoisomers by capillary electrophoresis with cyclodextrins J. Chromatogr., 630(1-2), 353-61, 1992)

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