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Abstract
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.
Declaration of interest
The authors declare that there are no conflicts of interest. Tongyuan Lin and Xia Huang contributed equally to this work. This work was financially supported by National Special Science and Technology Major of “Significant New Drugs Innovation and Development” key Projects (2009ZX09103-399), Key University natural science research project of Anhui province (KJ2011A190).