PEG–lipid–PLGA hybrid nanoparticles loaded with berberine–phospholipid complex to facilitate the oral delivery efficiency

Figures & data

Table 1. Particle size and encapsulation efficiency of PEG–lipid–PLGA NPs/BBR–SPC at different weight ratios of the BBR–SPC complex to PLGA polymer.

NPs	BBR–SPC:PLGA (mass ratio)	Initial drug amount (mg)	Particle size (nm)	Encapsulation efficiency (%)
PEG–lipid–PLGA NPs/BBR	–	2	173.1 ± 3.3	36.7 ± 3.4
PEG–lipid–PLGA NPs/BBR–SPC	1:8	2	161.2 ± 2.9	90.1 ± 6.2
PEG–lipid–PLGA NPs/BBR–SPC	1:4	4	149.6 ± 5.1	89.5 ± 4.6
PEG–lipid–PLGA NPs/BBR–SPC	1:2	8	151.2 ± 6.4	56.2 ± 5.9

Figure 1. Schematic illustration of the preparation of PEG–lipid–PLGA NPs/BBR–SPC for oral drug delivery.

Figure 2. Characterization of PEG–lipid–PLGA NPs/BBR–SPC. (A) Schematic structure, (B) TEM image, (C) SEM image, (D) particle size distribution and (E) zeta potential of PEG–lipid–PLGA NPs/BBR–SPC.

Table 2. Stability studies of PEG–lipid–PLGA NPs/BBR–SPC at SGF and SIF.

	Size (nm)		Drug encapsulation efficiency (%)
Parameters	Initial	Final	Initial	Final
SGF pH 1.2	155.6 ± 8.10	152.6 ± 8.51	89.5 ± 4.6	76.05 ± 1.02
SIF pH 6.8	152.6 ± 4.33	145.5 ± 6.46	89.5 ± 4.6	82.91 ± 2.16

Figure 3. DSC and XRD of the PEG–lipid–PLGA NPs/BBR-SPC. (A) DSC and (B) XRD of BBR, SPC, BBR + SPC, BBR–SPC, PEG–lipid–PLGA NPs, a physical mixture of all ingredients and PEG–lipid–PLGA NPs/BBR–SPC.

Figure 4. In vitro time-dependent drug release profiles of BBR and PEG–lipid–PLGA NPs/BBR–SPC in (A) SGF and (B) SIF.

Figure 5. CLSM images of different segments of the small intestine. CLSM images showing the absorption of (A) BBR and (B) PEG–lipid–PLGA NPs/BBR–SPC in different segments of the small intestine. DAPI was used to label the cell nuclei (blue).

Figure 6. The profiles of the plasma BBR level versus time among the rats after oral administration of BBR and PEG–lipid–PLGA NPs/BBR–SPC. The data are presented as the mean ± SD (n = 6).

Table 3. Pharmacokinetic parameters of various groups of rats after a single oral dose administration of BBR and the PEG–lipid–PLGA NPs/BBR–SPC.

	Unit	BBR	PEG–lipid–PLGA NPs/BBR–SPC
Dose	mg/kg	100	100
Cmax	ng/mL	116.09 ± 15.31	369.51 ± 9.10
Tmax	H	0.5	2
AUC	ng h/mL	1029.03 ± 126.02	3499.68  ± 220.21
BAR		–	3.43 ± 0.29

AUC: area under the BBR plasma concentration–time curve; BA_R: the relative bioavailability of the PEG–lipid–PLGA NPs/BBR–SPC compared with the oral administration of BBR group (n = 6 for each group).