Development of a Sustained-Release Voriconazole-Containing Thermogel for Subconjunctival Injection in Horses
| Autor: | Terri Hathcock, Anne A. Wooldridge, Rosemary Cuming, William R. Ravis, S. H. Duran, Eva Abarca, Yuh-Jing Lin, R. Jayachandra Babu, Allison J. Stewart |
|---|---|
| Rok vydání: | 2017 |
| Předmět: |
medicine.medical_specialty
food.ingredient Antifungal Agents 040301 veterinary sciences Polyesters Polyethylene Glycols 0403 veterinary science Cornea 03 medical and health sciences 0302 clinical medicine food In vivo Ophthalmology Medicine Agar Animals Tissue Distribution Horses Chromatography High Pressure Liquid Voriconazole Drug Carriers business.industry Temperature Horse 04 agricultural and veterinary sciences Permeation Sclera Disease Models Animal medicine.anatomical_structure Delayed-Action Preparations 030221 ophthalmology & optometry Injections Intraocular business Conjunctiva Eye Infections Fungal Gels Ex vivo medicine.drug Aspergillus flavus |
| Zdroj: | Investigative ophthalmologyvisual science. 58(5) |
| ISSN: | 1552-5783 |
| Popis: | PURPOSE. To determine in vitro release profiles, transcorneal permeation, and ocular injection characteristics of a voriconazole-containing thermogel suitable for injection into the subconjunctival space (SCS). METHODS. In vitro release rate of voriconazole (0.3% and 1.5%) from poly (DL-lactide-coglycolide-b-ethylene glycol-b-DL-lactide-co-glycolide) (PLGA-PEG-PLGA) thermogel was determined for 28 days. A Franz cell diffusion chamber was used to evaluate equine transcorneal and transscleral permeation of voriconazole (1.5% topical solution, 0.3% and 1.5% voriconazole-thermogel) for 24 hours. Antifungal activity of voriconazole released from the 1.5% voriconazole-thermogel was determined via the agar disk diffusion method. Ex vivo equine eyes were injected with liquid voriconazole-thermogel (4°C). Distension of the SCS was assessed ultrasonographically and macroscopically. SCS voriconazole-thermogel injections were performed in a horse 1 week and 2 hours before euthanasia and histopathologic analysis of ocular tissues performed. RESULTS. Voriconazole was released from the PLGA-PEG-PLGA thermogel for more than 21 days in all groups. Release followed first-order kinetics. Voriconazole diffused through the cornea and sclera in all groups. Permeation was greater through the sclerae than corneas. Voriconazole released from the 1.5% voriconazole-thermogel showed antifungal activity in vitro. Voriconazole-thermogel was easily able to be injected into the dorsal SCS where it formed a discrete gel deposit. Voriconazole-thermogel was easily injected in vivo and did not induce any adverse reactions. CONCLUSIONS. Voriconazole-containing thermogels have potential application in treatment of keratomycosis. Further research is required to evaluate their performance in vivo. |
| Databáze: | OpenAIRE |
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