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OBJECTIVE To preparet aurocholic acid modified PLGA nanospheres for oral delivery of semaglutide. METHODS The nanospheres were prepared by dobule emulsion solvent evaporation technique, and the preparation process was optimized by single-factor experiments; the nanospheres were characterized by scanning electron microscopy, Fourier transform infrared spectroscopy and laser particle size measurement; pharmacokinetic experiments were performed using SD rats; pharmacodynamic experiments were performed using db/db mice. RESULTS The FT-IR showed that taurocholic acid was successfully modified to the surface of the nanospheres. The particle size of the nanospheres was (185.9±3.31) nm, the ζ-potential was (-32.53±0.95) mV, and the drug loading and encapsulation rates were (11.15±0.07)% and (85. 51±0.01)%. The nanospheres showed good sustained release in vitro, with a cumulative release rate of 84. 96% within 192 h. Pharmacokinetic experiments were performed in SD rats, and the results showed that the bioavailability of nanospheres was 2.5%, and the slow release of semaglutide could be achieved within 192 h. The efficacy of nanospheres was verified in db/db mice, and the results showed that after gavage administration of nanospheres, the blood glucose of diabetic mice decreased rapidly and remained stable for about 3 d. CONCLUSION The oral delivery of semaglutide nanospheres prepared in this study has high drug loading and encapsulation efficiency, which can effectively control the blood glucose of diabetic mice within 3 d and improve the bioavailability.
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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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