TY - JOUR
T1 - Investigation of size, surface charge, PEGylation degree and concentration on the cellular uptake of polymer nanoparticles
AU - Ferrari, Raffaele
AU - Lupi, Monica
AU - Colombo, Claudio
AU - Morbidelli, Massimo
AU - D'Incalci, Maurizio
AU - Moscatelli, Davide
PY - 2014/11/1
Y1 - 2014/11/1
N2 - In this work a large number of polymer nanoparticles (NPs) with different features have been synthesized through emulsion polymerization-based methods. Poly(methyl methacrylate) (PMMA), poly-e{open}-caprolactone (PCL), and poly(lactic acid) (PLA) based NPs with different size, hydrophobicity, surface charge, PEGylation degree, type of emulsifier and ζ potential have been produced and characterized. All the different NPs have been adopted for cellular uptake studies, leading to a precise quantification of the number of internalized NPs into a selected tumor cell line. The experiments summarize, emphasize and improve the comprehension of the influence of NPs features on the uptake efficiency. In detail, a linear relationship between uptake and both size and NP concentration independently upon other NP characteristics was found. Moreover, it was confirmed that cells are able to internalize and retain for a long time preferentially positively charged NPs. Finally, by coupling results of uptake studies with cell viability measurements, an easy and fast check to control the effectiveness of a selected polymer as drug carrier has been proposed. In particular, we observed that biodegradable PLA-based NPs with high molecular weight, non-PEGylated and positively charged PCL NPs are the better choice to maximize the uptake and minimize side effect against cells.
AB - In this work a large number of polymer nanoparticles (NPs) with different features have been synthesized through emulsion polymerization-based methods. Poly(methyl methacrylate) (PMMA), poly-e{open}-caprolactone (PCL), and poly(lactic acid) (PLA) based NPs with different size, hydrophobicity, surface charge, PEGylation degree, type of emulsifier and ζ potential have been produced and characterized. All the different NPs have been adopted for cellular uptake studies, leading to a precise quantification of the number of internalized NPs into a selected tumor cell line. The experiments summarize, emphasize and improve the comprehension of the influence of NPs features on the uptake efficiency. In detail, a linear relationship between uptake and both size and NP concentration independently upon other NP characteristics was found. Moreover, it was confirmed that cells are able to internalize and retain for a long time preferentially positively charged NPs. Finally, by coupling results of uptake studies with cell viability measurements, an easy and fast check to control the effectiveness of a selected polymer as drug carrier has been proposed. In particular, we observed that biodegradable PLA-based NPs with high molecular weight, non-PEGylated and positively charged PCL NPs are the better choice to maximize the uptake and minimize side effect against cells.
KW - Drug delivery
KW - Endocytosis
KW - Imaging
KW - Nanoparticle
KW - Polymer
KW - Uptake
UR - http://www.scopus.com/inward/record.url?scp=84915778929&partnerID=8YFLogxK
UR - http://www.scopus.com/inward/citedby.url?scp=84915778929&partnerID=8YFLogxK
U2 - 10.1016/j.colsurfb.2014.10.003
DO - 10.1016/j.colsurfb.2014.10.003
M3 - Article
AN - SCOPUS:84915778929
VL - 123
SP - 639
EP - 647
JO - Colloids and Surfaces B: Biointerfaces
JF - Colloids and Surfaces B: Biointerfaces
SN - 0927-7765
ER -