Evaluation of pullulan-functionalized doxorubicin nanoparticles for asialoglycoprotein receptor-mediated uptake in Hep G2 cell line

• Published in: Cancer nanotechnology Vol. 2; no. 1-6; pp. 49 - 55
• Main Authors: Guhagarkar, Swati A., Majee, Sharmila B., Samad, Abdul, Devarajan, Padma V.
• Format: Journal Article
• Language: English
• Published: Vienna Springer Vienna 2011; Springer Nature B.V
• Subjects: Biochemistry; Biomedical Engineering and Bioengineering; Cancer Research; Chemistry and Materials Science; Materials Science; Nanotechnology; Original Paper; Hep G2 cells; Asialoglycoprotein receptor; Pullulan; Polyethylene sebacate; Doxorubicin
• ISSN: 1868-6958; 1868-6966
• DOI: 10.1007/s12645-011-0012-x

The present study discusses evaluation of pullulan-functionalized doxorubicin nanoparticles for asialoglycoprotein receptor-mediated uptake in the Hep G2 cell line. Doxorubicin hydrochloride (DOX) nanoparticles using polymers of different hydrophobic character, polyethylene sebacate (hydrophobic) and poly (lactic-co-glycolic acid) (intermediate hydrophobicity) with high entrapment efficiency and particle size were prepared by modified nanoprecipitation, using Gantrez AN 119 as complexing agent. Nanoparticles of Gantrez AN 119 were also prepared to represent a hydrophilic polymer. Cell uptake of DOX nanoparticles was found to be comparable to DOX solution irrespective of DOX concentration, nanoparticles size, and pullulan concentration. Furthermore, uptake of nanoparticles functionalized with or without pullulan prepared with polymers of different hydrophobic character revealed comparable uptake. Comparable uptake of DOX solution and DOX nanoparticles functionalized with or without pullulan suggest extracellular release of DOX as the mechanism of uptake from the nanoparticles. In vivo evaluation in hepatic cancer model is therefore essential to confirm the role of pullulan as asialoglycoprotein receptors ligand.