Nose-to-brain delivery of borneol modified tanshinone IIA nanoparticles in prevention of cerebral ischemia/reperfusion injury. (1st January 2021)

• Record Type: Journal Article
• Authors: Wang, Luting; Xu, Lin; Du, Junfeng; Zhao, Xiao; Liu, Mei; Feng, Jianfang; Hu, Kaili
• Is Part Of: Drug delivery. Volume 28:Number 1(2021)
• Page Start: 1363
• Page End: 1375
• Publication Date: 2021-01-01
• Subjects: PEG–PLGA nanoparticles -- borneol -- tanshinone IIA -- intranasal delivery -- cerebral ischemia/reperfusion injury; Drug delivery systems -- Periodicals; Drug targeting -- Periodicals; 615.05
• DOI: 10.1080/10717544.2021.1943058
• Languages: English
• ISSNs: 1071-7544

Abstract

Abstract: Targeted treatment of cerebral ischemia/reperfusion injury (CIRI) remains a problem due to the difficulty in drug delivery across the blood–brain barrier (BBB). In this study, we developed Bo-TSA-NP, a novel tanshinone IIA (TSA) loaded nanoparticles modified by borneol, which has long been proved with the ability to enhance other drugs' transport across the BBB. The Bo-TSA-NP, with a particle size of about 160 nm, drug loading of 3.6%, showed sustained release and P-glycoprotein (P-gp) inhibition property. It demonstrated a significantly higher uptake by 16HBE cells in vitro through the clathrin/caveolae-mediated endocytosis and micropinocytosis. Following intranasal (IN) administration, Bo-TSA-NP significantly improved the preventive effect on a rat model of CIRI with improved neurological scores, decreased cerebral infarction areas and a reduced content of malondialdehyde (MDA) and increased activity of superoxide dismutase (SOD) in rat brain. In conclusion, these results indicate that Bo-TSA-NP is a promising nose-to-brain delivery system that can enhance the prevention effect of TSA on CIRI.