Evaluation of Intestinal Absorption Mechanism and Pharmacokinetics of Curcumin-Loaded Galactosylated Albumin Nanoparticles

Figures & data

Figure 1 The cell viability of Cur and Gal-BSA-Cur NPs on Caco-2 cells.

Notes: Each point represents the mean ± standard deviation (n=6). **P < 0.01, ***P< 0.001, compared to Gal-BSA-Cur NPs.

Abbreviations: Cur, curcumin; Gal-BSA-Cur NPs, curcumin-loaded galactosylated BSA nanoparticles.

Figure 2 Fluorescence microscopy images of cells incubated with 25 μmol/L of Cur and Gal-BSA-Cur NPs for 4 hrs.

Notes: Scale bar: 50μm, Magnification ×400. DAPI: cell nuclei (blue), merged: fluorescence overlaid image.

Abbreviations: Cur, curcumin; Gal-BSA-Cur NPs, curcumin-loaded galactosylated BSA nanoparticles.

Figure 3 The quantitative assay of cellular uptake of Cur and Gal-BSA-Cur NPs in Caco-2 cells using HPLC.

Notes: The curcumin concentration was detected by HPLC. ***P <0.001 compared with Gal-BSA-Cur NPs. The results were expressed as the mean ± standard deviation (n=3).

Abbreviations: Cur, curcumin; Gal-BSA-Cur NPs, curcumin-loaded galactosylated BSA nanoparticles; HPLC, high-performance liquid chromatography.

Figure 4 Intracellular uptake of Cur and Gal-BSA-Cur NPs in Caco-2 cells pretreated with different inhibitors.

Notes: ***P <0.001 compared with Cur or Gal-BSA-Cur NPs. **P <0.01, compared to the pretreatment with sodium azide or sucrose. The results were expressed as the mean ± standard deviation (n=3).

Abbreviations: Cur, curcumin; Gal-BSA-Cur NPs, curcumin-loaded galactosylated BSA nanoparticles.

Figure 5 Scheme of the absorption mechanism used by Cur or Gal-BSA-Cur NPs.

Abbreviations: Cur, curcumin; Gal-BSA-Cur NPs, curcumin-loaded galactosylated BSA nanoparticles.

Figure 6 In vitro the Ussing chamber cumulative absorption of Cur and Gal-BSA-Cur NPs in rat jejunums (n=3).

Abbreviations: Cur, curcumin; Gal-BSA-Cur NPs, curcumin-loaded galactosylated BSA nanoparticles.

Table 1 The Apparent Permeability Values (p_app) of Cur and Gal-BSA-Cur NPs Determined from Ussing Chamber Assay in Mucosal-to-Serosal (M-S) and Serosal-to-Mucosal (S-M)

Groups	Papp (×10−^Citation7, cm • s−^Citation1)
Cur M-S	0.69±0.03
Cur S-M	0.27±0.01
Gal-BSA-Cur NPs M-S	1.04±0.01
Gal-BSA-Cur NPs S-M	0.26±0.00

Abbreviations: Cur, curcumin; Gal-BSA-Cur NPs, curcumin-loaded galactosylated BSA nanoparticles; M-S, mucosal-to-serosal; S-M, serosal-to-mucosal.

Table 2 Pharmacokinetic Parameters of Cur and Gal-BSA-Cur NPs

Parameter	Gal-BSA-Cur NPs	Cur
AUC (0–48 hrs)/(ng/mL*h).	1047.6±41.2	775.4±35.7
MRT(0–48 hrs)/h	22.6±0.4	21.7±0.8
Cmax(ng/mL)	48.7±7.4	25.2±7.0
Tmax/h	0.5	2

Abbreviations: Cur, curcumin; Gal-BSA-Cur NPs, curcumin-loaded galactosylated BSA nanoparticles; AUC, area under the curve; MRT, mean retention time; C_max, peak plasma concentration; T_max, time at peak concentration.

Figure 7 The plasma concentrations versus time curves of Cur and Gal-BSA-Cur NPs after oral administration in rats. (A) The time from 0 to 48 hrs. (B) The time from 0 to 4 hrs.

Notes: Rats were treated with Cur (40 mg/kg) or Gal-BSA-Cur NPs (equivalent to the Cur). Data were represented as mean ± SD (n=6).

Abbreviations: Cur, curcumin; Gal-BSA-Cur NPs, curcumin-loaded galactosylated BSA nanoparticles.

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