title: Pharmacokinetic and anti-inflammatory effects of sanguinarine solid lipid nanoparticles.
abstract: 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 AUC(0→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.
authors.affiliation: School of Pharmacy, Xi'an Jiaotong University, No. 76 Western Yanta Road, Xi'an City, Shaanxi Province, 710061, People's Republic of China.
authors.forename: Weifeng
authors.initials: W
authors.lastname: Li
authors.forename: Huani
authors.initials: H
authors.lastname: Li
authors.forename: Huan
authors.initials: H
authors.lastname: Yao
authors.forename: Qingli
authors.initials: Q
authors.lastname: Mu
authors.forename: Guilan
authors.initials: G
authors.lastname: Zhao
authors.forename: Yongmei
authors.initials: Y
authors.lastname: Li
authors.forename: Hua
authors.initials: H
authors.lastname: Hu
authors.forename: Xiaofeng
authors.initials: X
authors.lastname: Niu
mesh_terms: D000284:Administration, Oral; D000818:Animals; D000893:Anti-Inflammatory Agents / Q000008:administration & dosage / Q000097:blood / Q000737:chemistry / Q000493:pharmacokinetics*; D053119:Benzophenanthridines / Q000008:administration & dosage / Q000097:blood / Q000737:chemistry / Q000493:pharmacokinetics*; D001682:Biological Availability; D002626:Chemistry, Pharmaceutical; D004195:Disease Models, Animal; D004337:Drug Carriers; D018836:Inflammation Mediators / Q000097:blood; D015850:Interleukin-6 / Q000097:blood; D007546:Isoquinolines / Q000008:administration & dosage / Q000097:blood / Q000737:chemistry / Q000493:pharmacokinetics*; D008055:Lipids / Q000737:chemistry*; D008070:Lipopolysaccharides; D008297:Male; D051379:Mice; D053758:Nanoparticles; D009569:Nitric Oxide / Q000097:blood; D010316:Particle Size; D051381:Rats; D017207:Rats, Sprague-Dawley; D012772:Shock, Septic / Q000097:blood / Q000139:chemically induced / Q000276:immunology / Q000517:prevention & control*; D012995:Solubility; D014409:Tumor Necrosis Factor-alpha / Q000097:blood
chemical_list: D000893:Anti-Inflammatory Agents; D053119:Benzophenanthridines; D004337:Drug Carriers; D018836:Inflammation Mediators; D015850:Interleukin-6; D007546:Isoquinolines; D008055:Lipids; D008070:Lipopolysaccharides; D014409:Tumor Necrosis Factor-alpha; C577686:interleukin-6, mouse; D009569:Nitric Oxide; C005705:sanguinarine