Synthesis, biodistribution, and microsingle photon emission computed tomography (SPECT) imaging study of technetium-99m labeled PEGylated dendrimer poly(amidoamine) (PAMAM)-folic acid conjugates.
Three conjugates based on dendrimer PAMAM generation five were synthesized and radiolabeled successfully. To investigate their tumor targeting, the in vitro and in vivo stability, cell uptake, in vivo biodistribution, and micro-SPECT imaging were evaluated, respectively. The conjugate of (99m)Tc labeled PEGylated dendrimer PAMAM folic acid conjugate ((99m)Tc-G5-Ac-pegFA-DTPA) shows much higher uptake in KB cancer cells and accumulated more in the tumor area than that of the other two conjugates. The uptake in KB cells depends on the incubation time. The results of in vivo biodistribution agree with the data obtained from micro-SPECT imaging. These studies show that PEGylation of PAMAM dendrimer folic acid conjugate improves the tumor targeting. Folate-conjugated dendrimer maybe developed to be potential radiopharmaceuticals and targeted drug delivery systems.
Zhang
Yuanqing
Y
Shanghai Institute of Applied Physics, Chinese Academy of Sciences, 2019 Baojia Road, Shanghai 201800, China.
Sun
Yanhong
Y
Xu
Xiaoping
X
Zhang
Xuezhu
X
Zhu
Hua
H
Huang
Liliang
L
Qi
Yujin
Y
Shen
Yu-Mei
YM
D000818:Animals; D045744:Cell Line, Tumor; D050091:Dendrimers / Q000138:chemical synthesis / Q000737:chemistry / Q000493:pharmacokinetics*; D016503:Drug Delivery Systems; D004355:Drug Stability; D005492:Folic Acid / Q000031:analogs & derivatives* / Q000138:chemical synthesis / Q000737:chemistry / Q000493:pharmacokinetics*; D006801:Humans; D066298:In Vitro Techniques; D051379:Mice; D008807:Mice, Inbred BALB C; D008819:Mice, Nude; D009368:Neoplasm Transplantation; D011092:Polyethylene Glycols / Q000737:chemistry*; D019275:Radiopharmaceuticals / Q000138:chemical synthesis / Q000737:chemistry / Q000493:pharmacokinetics*; D013667:Technetium / Q000737:chemistry / Q000493:pharmacokinetics*; D014018:Tissue Distribution; D015899:Tomography, Emission-Computed, Single-Photon; D014183:Transplantation, Heterologous
D050091:Dendrimers; C104700:PAMAM Starburst; D019275:Radiopharmaceuticals; D011092:Polyethylene Glycols; D013667:Technetium; D005492:Folic Acid