Resveratrol eye drops as well as preparation method and application

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In some cases, the simplest, most straightforward ideas are the best. Why not develop an eye-drop based on cyclodextrin and resveratrol?  The resveratrol captured in an HPBCD inclusion complex has the advantages of simple preparation, short preparation period, no organic solvent residue, and no bacteriostatic agent. The lipoic acid added in the clathrate eye drops prepared by the invention cooperates with the resveratrol to play a better antioxidant effect so that the xerophthalmia is better relieved, and the treatment effect is achieved.

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Original paper: Espacenet – Resveratrol eye drops as well as preparation method and application thereof

Oral alpha-cyclodextrin reverses cholesterol-crystal-induced retinal pathology in a rodent model of type 2 diabetes

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Today’s cyclodextrin a study showing how alpha-CD treatment could be used in type-2 diabetes patients.
Cholesterol crystals were eliminated from the retinas of diabetic mice after oral alpha-cyclodextrin treatment. These findings demonstrate that T2D is associated with cholesterol crystal-induced retinal pathology that is improved using oral alpha-cyclodextrin. Improvements were observed in inflammation, neural function and visual response.

Oral alpha-cyclodextrin reverses cholesterol-crystal-induced retinal pathology in a rodent model of type 2 diabetes (T2D). | IOVS | ARVO Journals

Cyclodextrin-enabled nepafenac eye drops with improved absorption open a new therapeutic window

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This research is close to my heart as it comes from a Hungarian collaboration on developing nepafenac eyedrops with improved absorption. The results showed that one formulation possessed better bioavailability ex vivo than Nevanac® 0.1 % suspension, while the other formulation containing only 60 % of the original dose was ex vivo equivalent with Nevanac® opening the way to nepafenac-containing eye drops with better patient compliance in the future.

Anna Vincze, Facskó Réka, Budai-Szűcs Mária, Gábor Katona, Benjámin Gyarmati, Anita Csorba, Dr. Zelkó Romána, Zoltán Zsolt Nagy, Lajos Szente, György Tibor Balogh,

See the full article here.

Aldeyra Therapeutics Announces FDA Acceptance of New Drug Application for Reproxalap for the Treatment of Dry Eye Disease

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This is a long-awaited approval of the very first SBECD-enabled reproxalap ophthalmic formulation delivered by Aldeyra Therapeutics to treat dry eye disease.
Reproxalap, an investigational new drug candidate, is a first-in-class small-molecule modulator of RASP (reactive aldehyde species), which are elevated in ocular and systemic inflammatory disease. The mechanism of action of reproxalap has been supported by the demonstration of statistically significant and clinically relevant activity in multiple physiologically distinct late-phase clinical indications.
Dry eye disease is a common inflammatory disease estimated to affect 39 million or more adults in the United States. The disease is characterized by insufficient moisture and lubrication in the anterior surface of the eye, leading to dryness, inflammation, pain, discomfort, irritation, diminished quality of life, and in severe cases, permanent vision impairment. Among many physicians and patients, existing therapy for dry eye disease is generally regarded as inadequate and often requires weeks or months to demonstrate activity. In patients with dry eye disease, RASP may contribute to ocular inflammation, diminished tear production, ocular redness, and changes in tear lipid composition. By diminishing RASP levels, Aldeyra’s lead RASP modulator reproxalap represents a novel and differentiated approach for treating the symptoms and signs of dry eye disease.

See the full press release here


Voriconazole Eye Drops: Enhanced Solubility and Stability through Ternary Voriconazole/Sulfobutyl Ether β-Cyclodextrin/Polyvinyl Alcohol Complexes

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This is a wonderful example of how something known (voriconazole-CD formulation) could be turned into something innovative. Researchers from Chulalongkorn University and Iceland University developed voriconazole eyedrops which shows high mucoadhesion, sustained release, good ex vivo permeability through the porcine cornea, and no sign of irritation. The stability study revealed that VCZ eye drops provide a shelf-life of more than 2.5 years at room temperature, while a shelf-life of only 3.5 months was observed for the extemporaneous Vfend® eye drops.

Hay Man Saung Hnin Soe, Khanittha Kerdpol, Thorsteinn Loftsson Phatsawee Jansook et al