Novel Drug Delivery Systems to Augment Presbyopia Therapeutics Pipeline

Presbyopia is a common vision disorder that manifests with increasing age. With age, the ciliary muscles of the eye start losing their flexibility that leads to the eye lens losing its flexibility as well. The eye gradually loses its ability to focus light directly on to the retina, and the image ends up forming behind it. This results in poor visibility of objects that are close to the eye. The normal aging process that causes presbyopia cannot be stopped or reversed. However, it can be rectified by wearing contact lenses and eyeglasses, or via surgeries.

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Signs and symptoms associated with presbyopia are a difficulty in reading small prints, headaches, eye muscle fatigue, and eyestrain. One of its early signs is blurred vision while holding things at the normal reading distance. Working in dimly lit environments could exacerbate the condition. Its diagnosis is done based on the patient’s age and medical history. In case of premature presbyopia, medical history becomes more important as it may correlate with a systemic disease. Conditions, such as neurological and vascular diseases, trauma, and diabetes mellitus and certain drugs, may lead to premature presbyopia.

The treatment for presbyopia is based on ophthalmologists and optometrists’ recommendations. The initial treatment involves prescribing of near-vision optical aids, such as reading glasses, magnifying lenses, and monocles. Vison-correction surgeries are also used for the treatment for long-sightedness (another term for the condition), as is the experimental pharmaceutical approach. One of the investigational drugs in the presbyopia therapeutics pipeline is naphazoline. Other drugs, such as polyethylene glycol, pheniramine, and nepafenac, are being tried with alpha-1 agonists, as they reduce ciliary muscle spasm, vascular congestion, and pilocarpine-induced hyperemia, thereby treating excess pupil constriction.

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One of the key driving factors for the presbyopia therapeutics pipeline is the invention of novel drug delivery systems. For example, AcrySof IQ PanOptix Toric intraocular lens for presbyopia was launched by the eye care division of Novartis, which is seen as a significant development in the presbyopia treatment scene. This is indicated for adults who have undergone cataract surgery and wish to achieve independence from spectacles. Similarly, the U.S. Food and Drug Administration approved the Raindrop Near Vision Inlay to be implanted in the cornea for presbyopia correction, in 2016.

The presbyopia therapeutics pipeline is segmented by development phase, route of administration, and molecule type. One of the candidates in the pipeline is carbachol and brimonidine drops, being developed by Principal Investigator Almamoun Abdelkader of the Department of Ophthalmology, Faculty of Medicine, Al-Azhar University, Cairo. Carbachol is a positively charged quaternary ammonium compound and a synthetic choline ester. The effect of acetylcholine on nicotinic and muscarinic receptors is mimicked by carbachol, which is a parasympathomimetic compound. The intraocular pressure is ultimately reduced due to the induction of miosis in the eye.

Brimonidine is a selective alpha-2 adrenergic receptor agonist and an imidazole derivative. It binds to these receptors present on the presynaptic nerve endings of the dilator muscle, which inhibits the neurotransmitter release into the synaptic cleft. This reduces the activity of the dilator muscle, thereby leading to a more-mitotic pupil. The production of aqueous humor is decreased due to the action of this compound on blood vessels, which causes them to constrict.

Therefore, as more such combination therapies are devised, people suffering from presbyopia might not have such a hard time in the coming years.

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