Photosensitizer Chlorin e6 Internalization into Tumor Cells in Phospholipid Nanoparticles Conjugated with Peptide Containing the NGR Sequence

  • V.N. Prozorovskiy Institute of Biomedical Chemistry, 10 Pogodinskaya str., Moscow, 119121 Russia
  • L.V. Kostryukova Institute of Biomedical Chemistry, 10 Pogodinskaya str., Moscow, 119121 Russia
  • E.I. Korotkevich Institute of Biomedical Chemistry, 10 Pogodinskaya str., Moscow, 119121 Russia
  • T.I. Torkhovskaya Institute of Biomedical Chemistry, 10 Pogodinskaya str., Moscow, 119121 Russia; Federal Research and Clinical Center of Physical-Chemical Medicine of Federal Medical Biological Agency, 1a Pirogovskaya str., Moscow, 119221 Russia
  • G.E. Morozevich Institute of Biomedical Chemistry, 10 Pogodinskaya str., Moscow, 119121 Russia
  • E.G. Tikhonova Institute of Biomedical Chemistry, 10 Pogodinskaya str., Moscow, 119121 Russia
  • O.M. Ipatova Institute of Biomedical Chemistry, 10 Pogodinskaya str., Moscow, 119121 Russia
Keywords: NGR; aminopeptidase N; MCF-7; HepG2; phospholipid nanoparticles; chlorin e6


The possibility of increased internalization of the photosensitizer chlorin e6 in tumor cells was investigatedusing soy phosphatidylcholine nanoparticles 20-30 nm with or without attached peptide containing Asn-Gly-Arg (NGR) motif was studied. This amino acid sequence exhibits affinity to aminopeptidase N (CD13), wich is overexpressed in a number of tumor cells and vessels. Nanoparticles with chlorin e6 were prepared with added of distearoylphosphatidylcholine (DSPE) conjugated through PEG with a hexapeptide containing the NGR sequence, and then were incubated with tumor cells НерG2 and MCF-7. Chlorin e6 accumulation in СD13-negative cells (MCF-7) did not depend on the presence of peptide NGR in nanoparticles. However, for НерG2 cells a twofold increase of chlorine e6 internalization was observed as compared with the same particles without NGR. Differences in the response of these two cell lines, differed in expression of aminopeptidase N (APN), suggest the possibility of this protein using for targeted delivery. The prospectivity of usage of phospholipids nanoparticles conjugated with targeting peptide for photodynamic therapy is discussed, taking into account possible variation of APN expression, inherent for many solid tumors.


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Experimental Research