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 ac...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.展开更多
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)+1 种基金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).
文摘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.
