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Merck

Biocompatible microemulsion modifies the tissue distribution of doxorubicin.

Journal of pharmaceutical sciences (2014-08-08)
Caroline Damico Candido, Michel Leandro Campos, Juliana Uruguay Correa Vidigal Assumpção, Kelly Chrystina Pestana, Elias Carvalho Padilha, Iracilda Zeppone Carlos, Rosângela Gonçalves Peccinini
要旨

The incorporation of doxorubicin (DOX) in a microemulsion (DOX-ME) has shown beneficial consequences by reducing the cardiotoxic effects of DOX. The aim of this study was to determine the distribution of DOX-ME in Ehrlich solid tumor (EST) and the heart, and compare it with that of free DOX. The distribution study was conducted with female Swiss mice with EST (n = 7 per group; 20-25 g). Animals received a single dose (10 mg/kg, i.p.) of DOX or DOX-ME 7 days after tumor inoculation. Fifteen minutes after administration, the animals were sacrificed, and the tumor and heart tissues were taken for immediate analysis by ultra-performance liquid chromatography. No difference was observed in DOX concentration in tumor tissue between DOX and DOX-ME administration. However, the most remarkable result in this study was the statistically significant reduction in DOX concentration in heart tissue of animals given DOX-ME. Mean DOX concentration in heart tissue was 0.92 ± 0.54 ng mg(-1) for DOX-ME and 1.85 ± 0.34 ng mg(-1) for free DOX. In conclusion, DOX-ME provides a better tissue distribution profile, with a lower drug concentration in heart tissue but still comparable tumor drug concentration, which indicates that antitumor activity would not be compromised.

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製品内容

Sigma-Aldrich
コレステロール, Sigma Grade, ≥99%
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コレステロール, powder, BioReagent, suitable for cell culture, ≥99%
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メチルアミン 溶液, 2.0 M in THF
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オレイン酸ナトリウム, ≥99%
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コレステロール, from sheep wool, ≥92.5% (GC), powder
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メチルアミン 溶液, 33 wt. % in absolute ethanol ((denatured with 1% toluene))
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メチルアミン 溶液, 2.0 M in methanol
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SyntheChol® NS0サプリメント, 500 ×, synthetic cholesterol, animal component-free, aqueous solution, sterile-filtered, suitable for cell culture
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コレステロール、植物由来, SyntheChol®
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コレステロール 溶液, certified reference material, 10 mg/mL in chloroform
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メチルアミン 溶液, 40 wt. % in H2O
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オレイン酸ナトリウム, ≥95% (capillary GC)
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コレステロール, tested according to Ph. Eur.
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