title: Enhanced hepatic targeting, biodistribution and antifibrotic efficacy of tanshinone IIA loaded globin nanoparticles.
abstract: Tanshinone IIA (TA) has been recently used to treat liver diseases. However, the poor water solubility and fast metabolism obstruct TA in to be used for the treatment of liver diseases. To overcome this, TA was encapsulated into globin to form nanoparticles (TA-Gb-NPs) by our self-assembling method. We evaluated their biodistribution, pharmacokinetics, targeting ability to liver and antifibrotic effects. As a result, TA-Gb-NPs had a good hepatic targeting ability and achieved higher concentration and longer retention in liver than tanshinone IIA suspension (TA-S). Compared with TA-S, TA-Gb-NPs significantly improved serum biochemical parameters in thioacetamide (TAA) induced liver fibrosis mouse model. Furthermore, histological analysis of mouse liver slices revealed that TA-Gb-NPs could markedly reduce the fibrosis scores and attenuate the progression of the hepatic fibrosis. In conclusion, the TA-Gb-NPs may be a good candidate for the treatment of hepatic fibrosis.
authors.affiliation: State Key Laboratory of Pharmaceutical Biotechnology, School of Life Sciences, Nanjing University, Nanjing 210093, PR China; College of Biotechnology and Pharmaceutical Engineering, Nanjing Tech University, Nanjing 211816, PR China.
authors.forename: Zhengjie
authors.initials: Z
authors.lastname: Meng
authors.affiliation: State Key Laboratory of Pharmaceutical Biotechnology, School of Life Sciences, Nanjing University, Nanjing 210093, PR China.
authors.forename: Lingtong
authors.initials: L
authors.lastname: Meng
authors.affiliation: State Key Laboratory of Pharmaceutical Biotechnology, School of Life Sciences, Nanjing University, Nanjing 210093, PR China.
authors.forename: Kaikai
authors.initials: K
authors.lastname: Wang
authors.affiliation: School of Pharmaceutical Sciences, Nanjing Tech University, Nanjing 211816, PR China.
authors.forename: Jing
authors.initials: J
authors.lastname: Li
authors.affiliation: State Key Laboratory of Pharmaceutical Biotechnology, School of Life Sciences, Nanjing University, Nanjing 210093, PR China.
authors.forename: Xiaoli
authors.initials: X
authors.lastname: Cao
authors.affiliation: State Key Laboratory of Pharmaceutical Biotechnology, School of Life Sciences, Nanjing University, Nanjing 210093, PR China. Electronic address: wuj@nju.edu.cn.
authors.forename: Jinhui
authors.initials: J
authors.lastname: Wu
authors.affiliation: State Key Laboratory of Pharmaceutical Biotechnology, School of Life Sciences, Nanjing University, Nanjing 210093, PR China. Electronic address: huyiqiao@nju.edu.cn.
authors.forename: Yiqiao
authors.initials: Y
authors.lastname: Hu
mesh_terms: D045784:Abietanes / Q000493:pharmacokinetics / Q000494:pharmacology* / Q000633:toxicity; D000818:Animals; D002152:Calorimetry, Differential Scanning; D002626:Chemistry, Pharmaceutical; D016503:Drug Delivery Systems; D004355:Drug Stability; D005343:Fibrinolytic Agents / Q000493:pharmacokinetics / Q000494:pharmacology* / Q000633:toxicity; D005914:Globins / Q000493:pharmacokinetics / Q000494:pharmacology* / Q000633:toxicity; D066298:In Vitro Techniques; D008099:Liver / Q000187:drug effects*; D008103:Liver Cirrhosis / Q000139:chemically induced / Q000188:drug therapy; D008297:Male; D051379:Mice; D008813:Mice, Inbred ICR; D053758:Nanoparticles; D013853:Thioacetamide; D014018:Tissue Distribution; D014961:X-Ray Diffraction
chemical_list: D045784:Abietanes; D005343:Fibrinolytic Agents; C021751:tanshinone; D013853:Thioacetamide; D005914:Globins
keywords: Antifibrotic; Globin; Hepatic fibrosis; Nanoparticles; Tanshinone IIA