Full
Outline
To improve the oral bioavailability of abiraterone acetate (ABA), reduce the administered dose, and eliminate its significant food effect.
ABA-loaded lipid nanoemulsion (ABA-NE) was prepared by high-pressure homogenization. The formulation and process parameters were optimized through single-factor tests and orthogonal experimental design. The prepared ABA-NE was characterized for particle size, polydispersity index (PDI), zeta potential, and entrapment efficiency. A pharmacokinetic study in beagle dogs was conducted to compare the bioavailability of ABA-NE with that of the reference tablets.
The optimized ABA-NE appeared as a white, homogeneous emulsion with average particle size of (195.61±3.12) nm, PDI of (0.05±0.01), Zeta potential of -(48.17±2.64) mV, encapsulation efficiency of (95.76±1.59)% and drug loading capacity of (39.84±0.23) mg·mL-1. The pharmacokinetic study demonstrated that compared with the reference formulation, ABA-NE significantly increased the maximum plasma concentration (Cmax) and the area under the concentration-time curve (AUC). The oral relative bioavailability of ABA-NE was 16.06-fold higher than that of the reference tablets.
ABA-NE can significantly improve the oral bioavailability of ABA, which is expected to reduce the clinical dosage. It also provides a potential strategy for eliminating the effect of food. However, further experiments after meals are needed to verify this hypothesis.
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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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