Synthesis and in vitro cancer cell targeting of folate-functionalized biodegradable amphiphilic dendrimer-like star polymers

  • Cao W
  • Zhou J
  • Wang Y
 et al. 
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By coupling a well-defined PLLA star polymer with six carboxylic acid-terminated polyester dendrons based on 2,2-bis(hydroxymethyl)propionic acid, a biodegradable dendrimer-like star polymer (DLSP) with multiple carboxylic acid groups at the outer surface was successfully synthesized. Conjugation of amine-functionalized folic acids (FA) onto the DLSP yielded a folate-DLSP hybrid as a carrier for targeted drug delivery. The chemical structures were proven by proton nuclear magnetic resonance and size exclusion chromatography. The DLSPs could form unimolecular micelles with a mean particle size of about 18 nm, as determined by dynamic light scattering. Flow cytometry and confocal microscope studies revealed that the cellular uptake of the folate-DLSP hybrid against KB cells (overexpressed folate-receptor) was much higher than that of the neat DLSP (without FA) due to the folate receptor-mediated binding.

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  • Weiqiang Cao

  • Jing Zhou

  • Yong Wang

  • Lei Zhu

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