Enhanced hepatic targeting, biodistribution and antifibrotic efficacy of tanshinone IIA loaded globin nanoparticles

Eur J Pharm Sci. 2015 Jun 20:73:35-43. doi: 10.1016/j.ejps.2015.03.002. Epub 2015 Mar 10.

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.

Keywords: Antifibrotic; Globin; Hepatic fibrosis; Nanoparticles; Tanshinone IIA.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Abietanes / pharmacokinetics
  • Abietanes / pharmacology*
  • Abietanes / toxicity
  • Animals
  • Calorimetry, Differential Scanning
  • Chemistry, Pharmaceutical
  • Drug Delivery Systems
  • Drug Stability
  • Fibrinolytic Agents / pharmacokinetics
  • Fibrinolytic Agents / pharmacology*
  • Fibrinolytic Agents / toxicity
  • Globins / pharmacokinetics
  • Globins / pharmacology*
  • Globins / toxicity
  • In Vitro Techniques
  • Liver / drug effects*
  • Liver Cirrhosis / chemically induced
  • Liver Cirrhosis / drug therapy
  • Male
  • Mice
  • Mice, Inbred ICR
  • Nanoparticles
  • Thioacetamide
  • Tissue Distribution
  • X-Ray Diffraction

Substances

  • Abietanes
  • Fibrinolytic Agents
  • tanshinone
  • Thioacetamide
  • Globins