Nanoemulsion-based delivery system for enhanced oral bioavailability and Caco-2 cell monolayers permeability of berberine hydrochloride

Figures & data

Figure 1. Plasma concentration profiles of BBH after oral administration of BBH nanoemulsion and BBH suspension in rats (n = 6).

Table 1. Pharmacokinetics parameters after oral administration of BBH nanoemulsion and BBH suspension to rats (n = 6).

Parameters	BBH suspension	BBH nanoemulsion
AUC(0–24) (mg/L h)	1.681 ± 0.558	4.963 ± 2.952
AUC(0–∞) (mg/L h)	2.223 ± 0.810	9.790 ± 8.410
MRT(0–24) (h)	10.009 ± 1.239	10.188 ± 2.391
MRT(0–∞) (h)	17.944 ± 6.357	21.020 ± 10.950
t1/2z (h)	9.761 ± 6.611	10.737 ± 7.027
Tmax (h)	1. 141 ± 1.469	4.778 ± 5.645
Cmax (mg L^−1)	0.259 ± 0.179	0.404 ± 0.13
Relative bioavailability		440.40%

Figure 2. Effect of BBH solution and BBH nanoemulsion on Caco-2 cells viability as evaluated by the MTT assay after 4 h.

Figure 3. Absorption concentration of BBH nanoemulsion and BBH nanoemulsion + Ver from A→B in Caco-2 cell model (n = 3).

Figure 4. Efflux concentration of BBH, BBH nanoemulsion, and BBH nanoemulsion + Ver from B→A in Caco-2 cell model (n = 3).

Table 2. Apparent permeability coefficients (P_app) and efflux ratio (ER) of BBH cross Caco-2 monolayer.

Group	Papp(A→B) (10^-8cm s^−1)	Papp(B→A) (10^-8cm s^−1)	ER
BBH	—	2.29 ± 0.11	—
BBH nanoemulsion	0.574 ± 0.18	1.76 ± 0.20**	3.07 ± 0.34
BBH nanoemulsion + Ver	0.185 ± 0.12*	1.07 ± 0.11#	5.78 ± 0.61^##

* p < .05, compared with BBH nanoemulsion in A to B transport.

** p < .01, compared with BBH in B to A transport.

# p < .01, compared with BBH nanoemulsion in B to A transport.

## p < .01, compared with BBH nanoemulsion.