The impact of PEGylation patterns on the in vivo biodistribution of mixed shell micelles.
Polyethylene glycol (PEG)-ylation is a widely used strategy to fabricate nanocarriers with a long blood circulation time. Further elaboration of the contribution of the surface PEGylation pattern to biodistribution is highly desirable. We fabricated a series of polyion complex (PIC) micelles PEGylated with different ratios (PEG2k and PEG550). The plasma protein adsorption, murine macrophage uptake, and in vivo biodistribution with iodine-125 as the tracer were systematically studied to elucidate the impact of PEGylation patterns on the biodistribution of micelles. We demonstrated that the PEGylated micelles with short hydrophilic PEG chains mixed on the surface were cleared quickly by the reticuloendothelial system (RES), and the single PEG2k PEGylated micelles could efficiently prolong the blood circulation time and increase their deposition in tumor sites. The present study extends the understanding of the PEGylation strategy to further advance the development of ideal nanocarriers for drug delivery and imaging applications.
Key Laboratory of Functional Polymer Materials, Ministry of Education, and Institute of Polymer Chemistry, Nankai University, Tianjin, People's Republic of China.
Hongjun
H
Gao
Jinjian
J
Liu
Cuihong
C
Yang
Tangjian
T
Cheng
Liping
L
Chu
Hongyan
H
Xu
Aimin
A
Meng
Saijun
S
Fan
Linqi
L
Shi
Jianfeng
J
Liu
D000327:Adsorption; D000704:Analysis of Variance; D000818:Animals; D001798:Blood Proteins / Q000378:metabolism; D002470:Cell Survival / Q000187:drug effects; D004337:Drug Carriers / Q000737:chemistry* / Q000493:pharmacokinetics* / Q000494:pharmacology; D056945:Hep G2 Cells; D006801:Humans; D007457:Iodine Radioisotopes / Q000737:chemistry / Q000493:pharmacokinetics; D008264:Macrophages / Q000378:metabolism; D051379:Mice; D008807:Mice, Inbred BALB C; D008823:Micelles; D008970:Molecular Weight; D041681:NIH 3T3 Cells; D053758:Nanoparticles / Q000737:chemistry; D010316:Particle Size; D011092:Polyethylene Glycols / Q000737:chemistry* / Q000493:pharmacokinetics* / Q000494:pharmacology; D014018:Tissue Distribution
D001798:Blood Proteins; D004337:Drug Carriers; D007457:Iodine Radioisotopes; D008823:Micelles; D011092:Polyethylene Glycols
PEGylation; drug delivery; in vivo biodistribution; macrophage uptake; mixed shell micelles