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M.N. Lott, M. Bartoli, S. Chamberlain, D. Chu, P. Bernstein, D.M. Marcus; Carotenoid–Mediated Retinal Delivery of Triamcinolone and Ketorolac . Invest. Ophthalmol. Vis. Sci. 2006;47(13):3803.
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Since the macula and retina preferentially concentrate carotenoids, we hypothesize that carotenoids will provide an ideal carrier for drug delivery to the retina. We synthesized a new class of drugs (consisting of triamcinolone and ketorolac linked chemically to zeaxanthin) and subsequently tested them in Japanese quail, a proven model for carotenoid studies.
Triamcinolone was esterified with zeaxanthin by dehydrating compounds. Free acid of ketorolac was esterified with the hydroxyl end of zeaxanthin. Six–week–old quail were then divided into the following groups: Control (n = 3) –– normal diet; IM (n = 4) –– normal diet and intramuscular zeaxanthin (0.7 mg 3X/wk for 6 wks); PO (n = 4) –– normal diet and oral zeaxanthin (0.7 mg 3X/wk for 6 wks); and XD (n = 4) –– diet without zeaxanthin or lutein. At week 12, tissues were harvested for HPLC quantification.
* Log transformation of data prior to ANOVA
** Retinal statistical significance unable to be performed due to only one control sample available
a, b = values with the same letter are not significantly different
These experiments demonstrate that a xanthophyll–deficient diet results in decreased tissue levels of zeaxanthin and lutein (statistically significant), obviating the need to breed quail for xanthophyll deficiency, as previously reported by others. In addition, oral administration of zeaxanthin may result in more efficient tissue delivery than IM administration (not statistically significant). Xanthophyll–deficient quail will be used to assess for oral carotenoid–mediated retinal delivery of triamcinolone and ketorolac.
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