A novel modified paclitaxel-loaded discoidal recombinant high-density lipoproteins: Preparation, characterizations and in vivo evaluation

Abstract

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 d-rHDLs (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 Sprague–Dawley 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.