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This study utilized monomethoxyl poly (ethylene glycol) 2000-poly (ε-caprolactone) 2000 (mPEG2K-PCL2K) and a self-synthesized functional carrier material, fructose-polyethylene glycol 2000-deoxycholic acid (Fru-PEG2K-DC), which targets the apical sodium-dependent bile acid transporter (ASBT) and glucose transporter 5 (GLUT5) on intestinal epithelial cells, to construct fructose-polyethylene glycol 2000-deoxycholic acid-polymeric micelles/curcumin (FD-PMs/Cur) with the aim of improving drug transintestinal transport efficiency. First, Fru-PEG2K-DC was synthesized via an azide-alkyne click chemical reaction, and the structure of the synthesized product was confirmed by nuclear magnetic resonance (NMR) and infrared spectroscopy (IR). Subsequently, the film dispersion method was employed to prepare curcumin-loaded targeted micelles. The preparation process and formulation of the drug-loaded nanomicelles were optimized and screened based on evaluation indicators such as particle size, polymer dispersity index (PDI), encapsulation efficiency, and drug loading capacity. Finally, in vitro cell experiments were conducted to evaluate the cellular uptake of the constructed targeted formulation and lysosomal escape function. The prepared FD-PMs/Cur exhibited a near-spherical shape, uniform size, and good dispersibility, with an average particle size of 25.86 ± 0.160 4 nm, PDI of 0.169 ± 0.015, and surface charge of -5.74 ± 0.707 mV. The encapsulation efficiency and drug loading capacity were (92.31 ± 0.40)% and (7.69 ± 0.04)%, respectively. The micelles demonstrated slow release and high stability in gastrointestinal fluids. In vitro cell experiments revealed that the targeted micelles significantly enhanced cellular uptake compared to free drugs and non-targeted micelles, indicating excellent intestinal targeting ability and lysosomal escape function. The constructed FD-PMs/Cur exhibited good gastrointestinal stability, intestinal epithelial cell-targeting capability and lysosomal escape function, effectively enhancing transintestinal transport efficiency. This study provides a novel strategy for improving the oral bioavailability of lipophilic drugs.
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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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