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      Call for Papers: Real-World Data as a Gold Mine

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      About Ophthalmologica: 2.1 Impact Factor I 5.1 CiteScore I 0.992 Scimago Journal & Country Rank (SJR)

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      Eine neue Plattform zum nicht invasiven Einbringen schlecht wasserlöslicher Substanzen ins Auge

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          Abstract

          To this day, the use of oily eye drops and non-invasive retinal delivery remain a major challenge. Oily eye drops usually cause ocular irritation and interfere with the normal functioning of the eye, while ocular injections for retinal drug delivery cause significant adverse effects and a high burden on the healthcare system. Here, the authors report a novel topical non-invasive ocular delivery platform (NIODP) through the periorbital skin for high-efficiency anterior and posterior ocular delivery in a non-human primate model (NHP). A single dose of about 7 mg JV-MD2 (omega 3 DHA) was delivered via the NIODP and reached the retina at a Cmax of 111 μg/g and the cornea at a Cmax of 66 μg/g. The NIODP also delivered JV-DE1, an anti-inflammatory agent in development for dry eye diseases, as efficiently as eye drops did to the anterior segments of the NHP. The topical NIODP seems to transport drug candidates through the corneal pathway to the anterior and via the conjunctiva/sclera pathway to the posterior segments of the eye. The novel NIODP method has the potential to reshape the landscape of ocular drug delivery. This is especially the case for oily eye drops and retinal delivery, where the success of the treatment lies in the ocular tolerability and bioavailability of drugs in the target tissue.

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          A Highly Effective and Ultra-Long-Acting Anti-Glaucoma Drug, with a Novel Periorbital Delivery Method.

          Purpose: Two features define the future of glaucoma therapeutics: (1) greatly improved ocular hypotensive efficacy and (2) a delivery method that improves patient convenience and compliance. A highly efficacious and extraordinarily long-acting ocular hypotensive agent PGN 9856-isopropyl ester represents a potential next-generation anti-glaucoma drug. A new periorbital drug delivery route was also investigated. Methods: PGN 9856-isopropyl ester pharmacology was determined by employing human cells, including prostanoid receptor transfectants, and FLIPr or cellular dielectric spectroscopy technology. Intraocular pressure (IOP) was measured in conscious cynomolgus monkeys trained to accept pneumatonometry when under gentle restraint. For periorbital application, the compound was applied radially using a roller-ball device connected to a cylindrical reservoir. Pharmacokinetic data were obtained using LC/MS/MS instrumentation. Results: Single doses of PGN 9856-isopropyl ester, administered over a 0.001%-0.01% dose range, produced profound decreases in monkey IOP that persisted for at least 5 days, which was long after the drug was detectable in ocular tissues. It was not uncommon for a single eye drop to reduce IOP to the level of 4-7 mm Hg. Drug application to the periorbital dermis of ocular normotensive monkeys produced a similarly profound reduction in IOP, which was well maintained. Conclusions: PGN 9856-isopropyl ester appears to possess efficacy and duration of action properties unmatched by currently prescribed anti-glaucoma agents and by those currently undergoing clinical evaluation. In addition, application to the periorbital skin using a roller-ball device offers a more convenient method of ophthalmic drug delivery than eye drops and is noninvasive, unlike other "dropless" technologies.
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            Discovery and potential utility of a novel non-invasive ocular delivery platform

              Author and article information

              Journal
              KOP
              10.1159/issn.2297-0118
              Kompass Ophthalmologie
              Kompass Ophthalmol
              S. Karger AG
              2297-0118
              2297-0045
              2024
              11 April 2024
              : 10
              : 2
              : 60-61
              Affiliations
              [ ]Experimentelle Ophthalmologie, Klinik für Augenheilkunde, Charité – Universitätsmedizin Berlin, Corporate Member of Freie Universität, Berlin Institute of Health, Humboldt-University, Berlin, Deutschland
              Author notes
              *Olaf Strauß, olaf.strauss@charite.de
              Article
              538628 Kompass Ophthalmol 2024;10:60–61
              10.1159/000538628
              2b611b8c-13f2-47b6-8ae3-b42bc4660807
              © 2024 S. Karger GmbH, Freiburg
              History
              Page count
              Pages: 2
              Categories
              Wissenstransfer

              Medicine
              drug delivery,ocular disease,oily eye drops,omega 3,retina,retinal delivery,retinal diseases,AMD,cornea,docosahexaenoic acid (DHA),non-invasive ocular delivery platform (NIODP)

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