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In order to improve the oral bioavailability of curcumin, curcumin nanocrystalline suspension (Cur-NCS) was prepared by the high-pressure homogenization method in "top-down" method. Its physical properties, in vitro release, in vivo bioavailability and anti-inflammatory activity were studied.
The prescription and process parameters were optimized using particle size and zeta potential as evaluation indexes; the sample morphology was characterized by transmission electron microscopy, the in vitro release of curcumin nanocrystallines suspension was determined by HPLC, and the blood concentration of curcumin in rats was measured by LC-MS/MS; the anti-inflammatory activity was investigated in RAW264.7 inflammatory cell model, and curcumin was investigated in a mouse model of bronchial asthma airway inflammation nanosuspension on the therapeutic effect of curcumin on airway inflammation in mice.
Preparation process: curcumin was sheared at high speed for 2 min at 16 000 r·min-1 and cycled 40 times at 800 bar. Prescription: curcumin dosage was 0.2%, TPGS dosage was 0.20% and soy lecithin dosage was 0.16%; the cumulative drug release of API and Cur-NCS was 11.67% and 27.44%, respectively. After gavage in rats, Cur-NCS bioavailability was increased by 1.86-fold after gavage in rats. In an in vitro inflammatory cell model and in vivo bronchial asthma mouse model, Cur-NCS significantly inhibited the expression of inflammatory factors NO, IL-6, TNF-α and the levels of MDA, IgE and ICAM-1, and increased the expression of IL-10 and the level of SOD.
The identified preparation process and prescription can meet the preparation requirements of curcumin nanosuspension, and the in vitro release, in vivo bioavailability and anti-inflammatory activity are significantly better than those of API, and curcumin nanosuspension can provide ideas for subsequent dosage form studies.
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| 科 Family | 属数 Number of genus | 种数 Number of species | 占总种数比例 Percentage of total species (%) | 属 Genus | 种数 Number of species | 占总种数比例 Percentage of total species (%) |
|---|---|---|---|---|---|---|
| 鹅膏菌科Amanitaceae | 2 | 11 | 5.26 | 鹅膏菌属 Amanita | 10 | 4.78 |
| 小菇科 Mycenaceae | 2 | 12 | 5.74 | 丝盖伞属 Inocybe | 5 | 2.39 |
| 多孔菌科 Polyporaceae | 8 | 14 | 6.70 | 蜡蘑属 Laccaria | 5 | 2.39 |
| 红菇科 Russulaceae | 3 | 23 | 11.00 | 小皮伞属 Marasmius | 6 | 2.87 |
| 小菇属 Mycena | 11 | 5.26 | ||||
| 光柄菇属 Pluteus | 5 | 2.39 | ||||
| 红菇属 Russula | 17 | 8.13 | ||||
| 栓菌属 Trametes | 5 | 2.39 |
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