Long circulation nanostructured lipid carriers for gambogenic acid: formulation design, characterization, and pharmacokinetic

Figures & data

Figure 1. The structure of GNA.

Figure 2. Transmission electron microscopy micrographs of NLCs: (A and B) GNA-NLC and (C and D) GNA-PEG–NLC.

Figure 3. (A–C) DSC curves of each the components of the formulations and GNA, and NLC formulations.

Figure 4. Release profiles of GNA from GNA-PEG-NLC and GNA-NLC in PBS pH 7.4 at 37 °C (n = 3).

Figure 5. Representative photomicrographs of vein damage caused by injection GNA-PEG–NLC (A), Blank PEG NLC (B), GNA-NLC (C), Blank NLC (D), GNA-solution (E), and PEG200 + 0.9% NaCl solution (F) (×100).

Figure 6. Mean concentration time profile of GNA in plasma following i.v. administration of a single dose of 1.0  mg/kg GNA-PEG-NLC, GNA-NLC, and GNA-solution to rats (n = 6).

Table 1. The main pharmacokinetic parameters of GNA of plasma following i.v. to rats (n = 6).

	Formulations
Pharmacokinetic parameters	GNA-solution	GNA-NLC	GNA-PEG-NLC
AUC0–t
mg/L min	2.17NLC71	12.68LC.47**	22.19LC.33#**
AUC0–∞
mg/L min	2.819LC91	13.28LC.05	25.83LC.73
MRT0–t
h	2.083LC20	3.363LC31**	3.983LC25##**
Cmax
μg/L	0.523LC61	1.273LC11	1.593LC92
Tmax
H	0.25	0.25	0.25

**p < 0.01 versus GNA solution.

## p < 0.01 versus GNA-NLC.

Figure 7. The AUC_0–t of GNA-solution, GNA-NLC, and GNA-PEG-NLC in tissue following i.v. to rats.

Figure 8. The Re values of GNA-NLC and GNA-PEG-NLC in tissue following i.v. to rats.