Body distribution and in situ evading of phagocytic uptake by macrophages of long-circulating poly (ethylene glycol) cyanoacrylate-co-nhexadecyl cyanoacrylate nanoparticles

作     者：Min HUANG Wei WU~2 Jun QIAN Dan-jing WAN Xiu-li WEI Jian-hua ZHU School of Pharmacy,Fudan University,Shanghai 200032,China 

作者机构：School of Pharmacy Fudan University Shanghai China 

出 版 物：《Acta Pharmacologica Sinica》 (中国药理学报(英文版))

年 卷 期：2005年第26卷第12期

页      面：1512-1518页

核心收录：

学科分类：1007[医学-药学(可授医学、理学学位)] 1006[医学-中西医结合] 100706[医学-药理学] 100602[医学-中西医结合临床] 10[医学] 

基　　金：Project supported by the Shanghai Municipal Committee of Science and Technology(Grant No 0243nm067) the Shanghai Education Bureau for Excellent Young High Education Teacher Candidates(Grant No 03YQHB008) 

主　　题：nanotechnology tissue distribution polyethylene glycols cynoacrylates polymers spleen 

摘      要：Aim:To investigate the body distribution in mice of[14C]-labeled polymethoxyethyleneglycol cyanoacrylate-co-n-hexadecyl cyanoacrylate(PEG-PHDCA)nanoparticles and in situ evading of phagocytic uptake by mouse peri-toneal ***:PEG-PHDCA copolymers were synthesized bycondensation of methoxypolyethylene glycol cyanoacetate with[14C]-hexadecyl-cyanoacetate.[14C]-nanoparticles were prepared using the nanoprecipitation/solvent diffusion method,while fluorescent nanoparticles were prepared by in-corporating rhodamine *** situ phagocytic uptake was evaluated by *** distribution in mice was evaluated by determining radioactivityin tissues using a scintillation ***:Phagocytic uptake by macroph-ages can be efficiently evaded by fluorescent PEG-PHDCA ***48 h,31% of the radioactivity of the stealth[14C]-PEG-PHDCA nanoparticles afteriv injection was still found in blood,whereas non-stealth PHDCA nanoparticleswere cleaned up from the bloodstream in a short *** distribution of stealthPEG-PHDCA nanoparticles and non-stealth PHDCA nanoparticals in mice waspoor in lung,kidney,and brain,and a little higher in *** accumula-tion was unusually high for both stealth and non-stealth nanoparticles,typical oflymphatic *** accumulation of stealth PEG-PHDCA nanoparticles in thespleen was 1.7 times as much as that of non-stealth PHDCA(P0.01).But theaccumulation of stealth PEG-PHDCA nanoparticles in the liver was 0.8 times asmuch as that of non-stealth PHDCA(P0.05).Conclusion:PEGylation leads tolong-circulation of nanoparticles in the bloodstream,and splenotropic accumula-tion opens up the potential for further development of spleen-targeted drug delivery.