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

1.?GNA-PEG-NLC and GNA-NLC were prepared by emulsification and low-temperature solidification methods. The optimized GNA-PEG-NLC and GNA-NLC were not only found to have small mean size (146.33?±?2.11 and 144.07?±?1.44) nm, high Zeta potential (?25.10?±?1.35 and ?28.03?±?0.29) mV, but also great entrapment efficiency (79.07?±?1.11 and 84.65?±?0.98%). TEM proved that particles were nearly spherical with smooth surface shape. Furthermore, in vitro release revealed a burst release initially, followed by a sustained profiles up to 48?h, and the cumulative drug release of GNA-PEG-NLC and GNA-NLC was 65.90?±?2.34% and 69.25?±?1.77%, respectively.

2.?In pharmacokinetic, GNA-PEG-NLC exhibited prolonged MRT and higher AUC values compared with GNA-NLC and GNA solution. Moreover, the tissue distribution demonstrated a high uptake of GNA-PEG-NLC in stomach.

3.?These results indicated that PEG-NLC is a promising delivery system for GNA, which could prolong drug circulation time in body and thus improved its bioavailability.