Chlorine e6 in Phospholipid Nanoparticles with Specific Targeting and Penetrating Peptides as Prospective Composition for Photodynamic Therapy of Malignant Neoplasms

• Published in: Biochemistry (Moscow). Supplement. Series B, Biomedical chemistry Biomedical chemistry, 2020-04, Vol.14 (2), p.174-179
• Main Authors: Kostryukova, L. V., Plyutinskaya, A. D., Pankratov, A. A., Korotkevich, E. I., Prozorovskiy, V. N., Tikhonova, E. G., Torkhovskaya, T. I., Teryoshkina, Yu. A.
• Format: Article
• Language: English
• Subjects: Bioorganic Chemistry; Chemistry; Chemistry and Materials Science; Chlorine; Cytotoxicity; Fibrosarcoma; Medicinal Chemistry; Nanoparticles; Peptides; Pharmacokinetics; Phospholipids; Photodynamic therapy
• ISSN: 1990-7508; 1990-7516
• DOI: 10.1134/S1990750820020080

Cytotoxic and photoinduced activity of chlorine e6 (Ce6) in phospholipid nanoparticles containing specific tumor targeting and cell-penetrating peptides was studied in vitro using human fibrosarcoma cells НТ-1080. It was shown, that addition of the cell-penetrating heptaarginine peptide (R7) alone or in combination with the peptide containing specific targeting motif NGR (Asn-Gly-Arg) resulted in a 3-fold increase of Ce6 photoinduced activity as compared with that in nanoparticles without peptides (the IC 50 values were 0.7 µg/mL and 2.1 µg/mL, respectively). A weak effect of NGR alone (less than 20%; IC 50 1.7 µg/mL) and the lack of its effect in addition to R7 (IC 50 0.7 µg/mL) suggest a greater importance of Ce6 penetration into cells rather than NGR-mediated targeting. The effect of inclusion of both peptides on the total cytotoxicity of Ce6 was minimal (10−16 times less than on the specific photoinduced activity). The results obtained in this study together with earlier shown effects on improvement of the pharmacokinetics of Ce6 in vivo after its inclusion into phospholipid nanoparticles indicate the prospects of using the obtained phospholipid nanoparticles system for photodynamic therapy.