Evaluation of brain targeting in rats of Salvianolic acid B nasal delivery by the microdialysis technique

Abstract

The purpose of this study was to investigate the biodistribution of Salvianolic acid B in rats blood and brain after intranasal administration and explore its feasibility and evaluate its brain targeting effect. The concentration of Salvianolic acid B in blood and brain following nasal administration (32 mgċkg⁻¹) was measured combining with microdialysis sampling and liquid chromatograph-mass spectrometer/MS detection technology. After the microdialysis samples were corrected with in vivo recoveries, the pharmacokinetic parameters were obtained by using non-compartment model and the brain targeting evaluated by the value of drug targeting index (DTI). The C_max in blood and brain by intravenous injection were higher than intranasal administration, but the intranasal administration of MRT_0-∞ significantly prolonged and increased by nearly 2.03 and 1.86 times, respectively. The DTI value of Salvianolic acid B was 5.54 and bioavailability (F) was 43.98%. After nasal administration of Salvianolic acid B, it has a certain brain targeting, which could become a new drug system for the treatment of brain diseases.

Keywords:

• Brain microdialysis
• LC-MS
• nasal administration
• pharmacokinetics
• Salvianolic acid B

Acknowledgments

The authors would like to acknowledge the Key Laboratory of basic and new drug research of traditional Chinese medicine in Shaanxi province and the third level laboratory of traditional Chinese Medicine preparation of national administration of TCM.

Declaration of interest

The authors report no conflicts of interest. The authors alone are responsible for the content and writing of this article.

This project was supported by the Key Research and Development Program of Shaanxi Province of China (No. 2017ZDXM-SF-008).