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.
a Pharmacokinetic Laboratory and Department of Clinical Pharmacy, Anhui University of Chinese Medicine , Hefei , China.
Tongyuan
T
Lin
a Pharmacokinetic Laboratory and Department of Clinical Pharmacy, Anhui University of Chinese Medicine , Hefei , China.
Xia
X
Huang
a Pharmacokinetic Laboratory and Department of Clinical Pharmacy, Anhui University of Chinese Medicine , Hefei , China.
Yanyan
Y
Wang
a Pharmacokinetic Laboratory and Department of Clinical Pharmacy, Anhui University of Chinese Medicine , Hefei , China.
Tingting
T
Zhu
a Pharmacokinetic Laboratory and Department of Clinical Pharmacy, Anhui University of Chinese Medicine , Hefei , China.
Qing
Q
Luo
a Pharmacokinetic Laboratory and Department of Clinical Pharmacy, Anhui University of Chinese Medicine , Hefei , China.
Xiaoxiao
X
Wang
a Pharmacokinetic Laboratory and Department of Clinical Pharmacy, Anhui University of Chinese Medicine , Hefei , China.
Kai
K
Zhou
a Pharmacokinetic Laboratory and Department of Clinical Pharmacy, Anhui University of Chinese Medicine , Hefei , China.
Hao
H
Cheng
a Pharmacokinetic Laboratory and Department of Clinical Pharmacy, Anhui University of Chinese Medicine , Hefei , China.
Daiyin
D
Peng
a Pharmacokinetic Laboratory and Department of Clinical Pharmacy, Anhui University of Chinese Medicine , Hefei , China.
Weidong
W
Chen
D004339:Drug Compounding / Q000379:methods*; D016503:Drug Delivery Systems; D008055:Lipids / Q000737:chemistry*; D049329:Nanostructures / Q000737:chemistry*; D014966:Xanthenes / Q000737:chemistry* / Q000493:pharmacokinetics
D008055:Lipids; D014966:Xanthenes; C045863:neo-gambogic acid
Bioavailability; PEG-modified nanostructured lipid carriers; gambogenic acid