Figures & data
Figure 1 Characterization of the natural nanoparticles (Nnps) isolated from Coptidis Rhizoma extract; (A) Content of Nnps in Coptidis Rhizoma extract; (B) Size and Zeta potential of Nnps; (C) Purity and molecular weight of the protein molecules (CRP, Coptidis Rhizoma protein) forming Nnps; (D) Scanning electron microscope observation of Nnps powder (10,000 ×); (E) Observation of Nnps powder by laser confocal fluorescence microscopy (6000 ×); (F) Observation of the water solution of Nnps by laser confocal fluorescence microscopy (6000 ×). In , the large red rectangle showed an enlarged image of the Nnps contained in the small red rectangle. In , the red dotted rectangle showed an enlarged image of the Nnps contained in the small red dotted circle, respectively.
Figure 2 Natural nanoparticles (Nnps) changed the crystal form of berberine hydrochloride (BBR). Scanning electron microscopy images of BBR (A) and Nnps-BBR (B) (10,000 ×); (C) Laser confocal fluorescence microscope observation (6000 ×) of BBR powder (a), BBR solution (b), Nnps-BBR powder (c), and Nnps-BBR solution (d); (D) Differential scanning calorimetry images of BBR, Nnps, the physical mixture of Nnps and BBR (Mix), and Nnps-BBR complex; (E) Powder X-ray diffraction images of BBR, Nnps, physical mixture of Nnps and BBR (Mix), and Nnps-BBR complex.
Figure 3 Effect of the natural nanoparticles (Nnps) on the solubility (A) and dissolution profile of berberine hydrochloride (BBR) in simulated gastric (B) or intestinal (C) fluid (Mean ± SD, n = 6). **p < 0.01 vs BBR.
Table 1 Effect of Natural Nanoparticles (Nnps) on the Apparent Permeability (Papp) and Efflux Rate (ER) of Berberine Hydrochloride (BBR) (Mean ± SD, n = 3)
Figure 4 Effect of the natural nanoparticles (Nnps) on the intestinal absorption of berberine hydrochloride (BBR) (Mean ± SD); (A) Effects of endocytosis inhibitors on the uptake of BBR (10 μg/mL) in Caco-2 cells (n = 3); (B) Absorption of BBR (10 mg/mL) in the gut sacs (n = 4); (C) Efflux of BBR (200 μg/mL) in the gut sacs in the presence or absence of 100 μg/mL verapamil (n = 4); (D) Elimination of BBR (10 μg/mL) in intestinal S9 (n = 3); (E) Elimination half-life of BBR (10 μg/mL) in intestinal S9 (n = 3); (F) Production of demethylberberine after BBR (10 μg/mL) was incubated with intestinal S9 (n = 3). AMI, amiloride (2.5 mM); BBR, berberine hydrochloride; CHL, chlorpromazine (10 μg/mL); CYT, cytochalasin D (5 μM); IND, indomethacin (100 μg/mL); Nnps, natural nanoparticles. A, * or **p < 0.01 vs Nnps. E, *p < 0.05 vs BBR.
Table 2 Pharmacokinetic Parameters of Berberine Hydrochloride (BBR) in the Systemic Circulation, Portal Vein, and Livers of Mice Receiving 200 mg/kg Oral BBR, The Complex of the Nanoparticles and BBR (Nnps-BBR), and Coptidis Rhizoma Extract, Which All Contained the Corresponding Dosage of BBR (Mean ± SD, n = 6)
Figure 5 Concentration-time curves of berberine hydrochloride (BBR) in the systemic circulation (A), portal vein (B), and livers (C) of mice receiving 200 mg/kg oral BBR, the complex of the natural nanoparticles (Nnps) and BBR (Nnps-BBR), and Coptidis Rhizoma extract, which all contained the corresponding dosage of BBR (Mean ± SD, n = 6).
