摘要
This study is one of the first to focus on the unexpected drug leakage from discoidal recombinant high-density lipoproteins(d-rHDLs)as a consequence of remodeling process,mainly associated with lecithin-cholesterol acyltransferase(LCAT)during their metabolic process.Here,a newly monocholesterylsuccinate(CHS)modified paclitaxel-loaded drHDLs(cP-d-rHDLs)were constructed successfully through structural modification,thus aiming to improve the performance of d-rHDLs.And next their in vitro physiochemical properties and pharmacokinetics in SpragueeDawley rats were elaborately investigated.Collectively our studies demonstrated that cP-d-rHDLs,whose remodeling behaviors were restrained effectively after structural modification,exhibited more excellent and promising properties as novel delivery vehicles for anti-cancer agents.
基金
This study is financially supported by National Science Foundation Grant of China(No.81072587)
Jiangsu Province Ordinary College and University Innovative Research Programs(No.CXZZ110805)
the Major Project of National Science and Technology of China for New Drugs Development(No.2009ZX09310-004)
the Special Found Project of Universities’Basic Scientific Research of Central Authorities(No.ZJ11253).