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Synthesis, biodistribution, and microsingle photon emission computed tomography (SPECT) imaging study of technetium-99m labeled PEGylated dendrimer poly(amidoamine) (PAMAM)-folic acid conjugates

Journal Article


Abstract


  • 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 99mTc labeled PEGylated dendrimer PAMAM folic acid conjugate (99mTc-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.

UOW Authors


  •   Zhang, Yuanqing (external author)
  •   Sun, Yanhong (external author)
  •   Xu, Xiaoping (external author)
  •   Zhang, Xuezhu (external author)
  •   Zhu, Hua (external author)
  •   Huang, Liliang (external author)
  •   Qi, Yujin
  •   Shen, Yu-Mei (external author)

Publication Date


  • 2010

Geographic Focus


Citation


  • Zhang, Y., Sun, Y., Xu, X., Zhang, X., Zhu, H., Huang, L., Qi, Y. & Shen, Y. (2010). Synthesis, biodistribution, and microsingle photon emission computed tomography (SPECT) imaging study of technetium-99m labeled PEGylated dendrimer poly(amidoamine) (PAMAM)-folic acid conjugates. Journal of Medicinal Chemistry, 53 (8), 3262-3272.

Scopus Eid


  • 2-s2.0-77951097615

Ro Metadata Url


  • http://ro.uow.edu.au/eispapers/957

Has Global Citation Frequency


Number Of Pages


  • 10

Start Page


  • 3262

End Page


  • 3272

Volume


  • 53

Issue


  • 8

Place Of Publication


  • United States

Abstract


  • 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 99mTc labeled PEGylated dendrimer PAMAM folic acid conjugate (99mTc-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.

UOW Authors


  •   Zhang, Yuanqing (external author)
  •   Sun, Yanhong (external author)
  •   Xu, Xiaoping (external author)
  •   Zhang, Xuezhu (external author)
  •   Zhu, Hua (external author)
  •   Huang, Liliang (external author)
  •   Qi, Yujin
  •   Shen, Yu-Mei (external author)

Publication Date


  • 2010

Geographic Focus


Citation


  • Zhang, Y., Sun, Y., Xu, X., Zhang, X., Zhu, H., Huang, L., Qi, Y. & Shen, Y. (2010). Synthesis, biodistribution, and microsingle photon emission computed tomography (SPECT) imaging study of technetium-99m labeled PEGylated dendrimer poly(amidoamine) (PAMAM)-folic acid conjugates. Journal of Medicinal Chemistry, 53 (8), 3262-3272.

Scopus Eid


  • 2-s2.0-77951097615

Ro Metadata Url


  • http://ro.uow.edu.au/eispapers/957

Has Global Citation Frequency


Number Of Pages


  • 10

Start Page


  • 3262

End Page


  • 3272

Volume


  • 53

Issue


  • 8

Place Of Publication


  • United States