Nose-to-brain delivery of borneol modified tanshinone IIA nanoparticles in prevention of cerebral ischemia/reperfusion injury

Drug Delivery

Junfeng Du¹  Lin Xu¹  Mei Liu¹  Xiao Zhao¹  Jianfang Feng¹  Luting Wang¹  Kaili Hu¹ 

[1] Institute of Interdisciplinary Integrative Medicine Research, Murad Research Center for Modernized Chinese Medicine, Shanghai University of Traditional Chinese Medicine;

关键词: peg–plga nanoparticles;    borneol;    tanshinone iia;    intranasal delivery;    cerebral ischemia/reperfusion injury;   

DOI  :  10.1080/10717544.2021.1943058

来源: DOAJ

【 摘 要 】

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.

【 授权许可】

Unknown