التفاصيل البيبلوغرافية
| العنوان: |
Development and Characterization of the Neuroregenerative Xanthohumol C/Hydroxypropyl- β -cyclodextrin Complex Suitable for Parenteral Administration. |
| المؤلفون: |
Kirchinger, Michael, Bieler, Lara, Tevini, Julia, Vogl, Michael, Haschke-Becher, Elisabeth, Felder, Thomas K., Couillard-Després, Sebastien, Riepl, Herbert, Urmann, Corinna |
| المصدر: |
Planta Medica; 2019, Vol. 85 Issue 16, p1233-1241, 9p |
| مصطلحات موضوعية: |
ANIMAL experimentation, CALORIMETRY, FLAVONOIDS, HIGH performance liquid chromatography, INTRAVENOUS therapy, MASS spectrometry, MOLECULAR structure, NEURODEGENERATION, NEURONS, RATS, SOLUBILITY, IN vitro studies, IN vivo studies |
| مستخلص: |
The chroman-like chalcone Xanthohumol C, originally found in hops, was demonstrated to be a potent neuroregenerative and neuroprotective natural product and therefore constitutes a strong candidate for further pharmaceutical research. The bottleneck for in vivo experiments is the low water solubility of this chalcone. Consequently, we developed and validated a suitable formulation enabling in vivo administration. Cyclodextrins were used as water-soluble and nontoxic complexing agents, and the complex of Xanthohumol C and 2-hydroxypropyl- β -cyclodextrin was characterized using HPLC, HPLC-MS, NMR, and differential scanning calorimetry. The water solubility of Xanthohumol C increases with increasing concentrations of cyclodextrin. Using 50 mM 2-hydroxypropyl- β -cyclodextrin, solubility was increased 650-fold. Furthermore, in vitro bioactivity of Xanthohumol C in free and complexed form did not significantly differ, suggesting the release of Xanthohumol C from 2-hydroxypropyl- β -cyclodextrin. Finally, a small-scaled in vivo experiment in a rat model showed that after i. p. administration of the complex, Xanthohumol C can be detected in serum, the brain, and the cerebrospinal fluid at 1 and 6 h post-administration. Mean (± SD) Xanthohumol C serum concentrations after 1, 6, and 12 h were determined as 463.5 (± 120.9), 61.9 (± 13.4), and 9.3 (± 0.8) ng/mL upon i. v., and 294.3 (± 22.4), 45.5 (± 0.7), and 13 (± 1.0) ng/mL after i. p. application, respectively. Accordingly, the formulation of Xanthohumol C/2-hydroxypropyl- β -cyclodextrin is suitable for further in vivo experiments and further pharmaceutical research aiming for the determination of its neuroregenerative potential in animal disease models. [ABSTRACT FROM AUTHOR] |
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| قاعدة البيانات: |
Complementary Index |
