TY - JOUR
T1 - Pharmacokinetic and anti-inflammatory effects of sanguinarine solid lipid nanoparticles
AU - Li, Weifeng
AU - Li, Huani
AU - Yao, Huan
AU - Mu, Qingli
AU - Zhao, Guilan
AU - Li, Yongmei
AU - Hu, Hua
AU - Niu, Xiaofeng
PY - 2014/4
Y1 - 2014/4
N2 - The sanguinarine (SG) was studied for its pharmacokinetic and anti-inflammatory activities with prepared solid lipid nanoparticles (SLNs). The sanguinarine solid lipid nanoparticles (SG-SLNs) were prepared by film-ultrasonic dispersion method and the entrapment efficiency of SG was higher at 75.6 %. The drug release profile of SG was examined in pH 7.4 PBS and 85 % of the SG loaded in SLNs was gradually released during 24 h. We used mice endotoxin shock model which was induced by lipopolysaccharide (1 mg/kg) to examine the anti-inflammatory function of SG-SLNs. Healthy Kunming mice were administered orally with saline, SG (10 mg/kg), and SG-SLNs (10 mg/kg), respectively, at 12 and 1 h before lipopolysaccharide (LPS) injection. Mice were sacrificed at 1 and 6 h, respectively, and blood was collect through the venous sinus to access inflammatory mediators. Pharmacokinetic studies proved that the AUC0→24 and C max of SG-SLNs were significantly increased compared that of SG. SG-SLNs revealed significant anti-inflammatory effects through inhibition of LPS-induced tumor necrosis factor-alpha level, interleukin 6 level, and nitric oxide production in serum. Therefore, it can be concluded that SG-SLNs led to a better oral bioavailability.
AB - The sanguinarine (SG) was studied for its pharmacokinetic and anti-inflammatory activities with prepared solid lipid nanoparticles (SLNs). The sanguinarine solid lipid nanoparticles (SG-SLNs) were prepared by film-ultrasonic dispersion method and the entrapment efficiency of SG was higher at 75.6 %. The drug release profile of SG was examined in pH 7.4 PBS and 85 % of the SG loaded in SLNs was gradually released during 24 h. We used mice endotoxin shock model which was induced by lipopolysaccharide (1 mg/kg) to examine the anti-inflammatory function of SG-SLNs. Healthy Kunming mice were administered orally with saline, SG (10 mg/kg), and SG-SLNs (10 mg/kg), respectively, at 12 and 1 h before lipopolysaccharide (LPS) injection. Mice were sacrificed at 1 and 6 h, respectively, and blood was collect through the venous sinus to access inflammatory mediators. Pharmacokinetic studies proved that the AUC0→24 and C max of SG-SLNs were significantly increased compared that of SG. SG-SLNs revealed significant anti-inflammatory effects through inhibition of LPS-induced tumor necrosis factor-alpha level, interleukin 6 level, and nitric oxide production in serum. Therefore, it can be concluded that SG-SLNs led to a better oral bioavailability.
KW - bioavailability
KW - inflammation
KW - inflammatory mediators
KW - sanguinarine
KW - solid lipid nanoparticles
UR - https://www.scopus.com/pages/publications/84896400535
U2 - 10.1007/s10753-013-9779-8
DO - 10.1007/s10753-013-9779-8
M3 - 文章
C2 - 24272172
AN - SCOPUS:84896400535
SN - 0360-3997
VL - 37
SP - 632
EP - 638
JO - Inflammation
JF - Inflammation
IS - 2
ER -