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I. Bravo-Osuna, R. Herrero-Vanrell, I. T. Molina Martínez, N. Girón, R. Gómez, F. de la Mata, M. Guzmán Navarro; In vitro and in vivo Tolerance Studies of Carbosilane Dendrimers for Ophthalmic Administration. Invest. Ophthalmol. Vis. Sci. 2010;51(13):437.
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© ARVO (1962-2015); The Authors (2016-present)
Background: The use of dendrimers in ophthalmology is currently one of the most stimulating working fields in drug delivery. In this mind, the objective of this work was the analysis of in-vitro and in-vivo tolerance of carbosilane dendrimers (anionic and cationic) for topical ophthalmic administration. Materials: First and third generation of carbosilane dendrimers (G1 and G3) were synthesised in the Dep. of Inorganic Chemistry, UAH, Spain.
2.5, 5 and 10 µM solutions of dendrimers in saline solution (SS) were evaluated according to MTT in-vitro test using conjunctiva (IOBA-NHC) and corneal (HCLE) cells. The contact time selected were 15minutes (short exposure), 1h and 4h (long exposure). The limit of acceptable cell survival was fixed at 80%, compared to survival of non-treated cells. In-vivo test was performed by instilling 25µl of dendrimer solutions on the right eye of four male New Zealand albino rabbits, using the left eye as control (instillation of SS) Experiments were conducted in compliance with the ARVO statements of the use of Animals in Ophthalmology and Vision Research. Evaluation (before instillation and 0h, 2h and 6h post-instillation), performed by biomicroscopy, implied: pupil reflex and size, superior and inferior eyelids, redness, blepharitis and blepharospasm, tear charge, exudates, TBUT, inflammation of nictitant membrane and cornea transparency.
In vitro tolerance studies
Both the in vitro and the in vivo tolerance studies performed demonstrated that carbosilane dendrimers are suitable for topical ophthalmic administration at 5-10µM.
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