bromohexadecanoyl paclitaxel conjugate 纳米非小细胞肺癌 原位.pdfVIP

International Journal of Nanomedicine Dovepress open access to scientific and medical research Open access Full Text article O r I g I N a l r e s e a r c h 2′-(2-bromohexadecanoyl)-paclitaxel conjugate nanoparticles for the treatment of non-small cell lung cancer in an orthotopic xenograft mouse model lei Peng 1 Abstract: A nanoparticle (NP) formulation with 2′-(2-bromohexadecanoyl)-paclitaxel a llison N schorzman2 (Br-16-PX) conjugate was developed in these studies for the treatment of non-small cell lung can- Ping Ma1 cer (NSCLC). The lipophilic paclitaxel conjugate Br-C16-PX was synthesized and incorporated a ndrew J Madden2 into lipid NPs where the 16-carbon chain enhanced drug entrapment in the drug delivery system William c Zamboni2–4 and improved in vivo pharmacokinetics. The electron-withdrawing bromine group was used to 1 facilitate the conversion of Br-C16-PX to paclitaxel at the tumor site. The developed system soumya rahima Benhabbour 1,4 was evaluated in luciferase-expressing A549 cells in vitro and in an orthotopic NSCLC mouse russell J Mumper model. The results demonstrated that the Br-C16-PX NPs had a higher maximum tolerated dose 1 center for Nanotechnology in (75 mg/kg) than Taxol® (19 mg/kg) and provided significantly longer median survival (88 days Drug Delivery, Division of Molecular Pha