{"status":"ok","message-type":"work","message-version":"1.0.0","message":{"indexed":{"date-parts":[[2026,5,29]],"date-time":"2026-05-29T19:25:22Z","timestamp":1780082722270,"version":"3.54.0"},"reference-count":75,"publisher":"MDPI AG","issue":"1","license":[{"start":{"date-parts":[[2024,1,18]],"date-time":"2024-01-18T00:00:00Z","timestamp":1705536000000},"content-version":"vor","delay-in-days":0,"URL":"https:\/\/creativecommons.org\/licenses\/by\/4.0\/"}],"funder":[{"name":"Russian Federation President\u2019s scholarship 2022\u20132023","award":["SP-3848.2022.4"],"award-info":[{"award-number":["SP-3848.2022.4"]}]}],"content-domain":{"domain":[],"crossmark-restriction":false},"short-container-title":["Pharmaceutics"],"abstract":"<jats:p>In this study, we described physico-chemical properties of novel nanoformulation of photosensitizer-pyropheophorbide \u03b1 17-diethylene glycol ester (XL) (chlorophyll \u03b1 derivative), revealing insights into antitumor activity and maintaining quality, meeting the pharmaceutical approach of new nanoformulation design. Our formulation, based on poly(lactic-co-glycolic acid) (PLGA) nanoparticles, increased XL solubility and selective tumor-targeted accumulation. In our research, we revealed, for the first time, that XL binding to polyvinyl alcohol (PVA) enhances XL photophysical activity, providing the rationale for PVA application as a stabilizer for nanoformulations. Results of FTIR, DSC, and XRD revealed the physical interactions between XL and excipients, including PVA, indicating that the encapsulation maintained XL binding to PVA. The encapsulated XL exhibited higher photophysical activity compared to non-encapsulated substance, which can be attributed to the influence of residual PVA. Gamma-irradiation led to degradation of XL; however, successful sterilization of the samples was achieved through the filtration. Importantly, the encapsulated and sterilized XL retained cytotoxicity against both 2D and 3D tumor cell models, demonstrating the potential of the formulated NP\u2013XL for photodynamic therapy applications, but lacked the ability to reactivate epigenetically silenced genes. These findings provide valuable insights into the design and characterization of PLGA-based nanoparticles for the encapsulation of photosensitizers.<\/jats:p>","DOI":"10.3390\/pharmaceutics16010126","type":"journal-article","created":{"date-parts":[[2024,1,18]],"date-time":"2024-01-18T11:28:46Z","timestamp":1705577326000},"page":"126","update-policy":"https:\/\/doi.org\/10.3390\/mdpi_crossmark_policy","source":"Crossref","is-referenced-by-count":11,"title":["Pharmaceutical Approach to Develop Novel Photosensitizer Nanoformulation: An Example of Design and Characterization Rationale of Chlorophyll \u03b1 Derivative"],"prefix":"10.3390","volume":"16","author":[{"given":"Maria B.","family":"Sokol","sequence":"first","affiliation":[{"name":"N. M. Emanuel Institute of Biochemical Physics of Russian Academy of Sciences, 119334 Moscow, Russia"}],"role":[{"vocabulary":"crossref","role":"author"}]},{"given":"Veronika A.","family":"Beganovskaya","sequence":"additional","affiliation":[{"name":"N. M. Emanuel Institute of Biochemical Physics of Russian Academy of Sciences, 119334 Moscow, Russia"}],"role":[{"vocabulary":"crossref","role":"author"}]},{"ORCID":"https:\/\/orcid.org\/0000-0002-9999-4652","authenticated-orcid":false,"given":"Mariia R.","family":"Mollaeva","sequence":"additional","affiliation":[{"name":"N. M. Emanuel Institute of Biochemical Physics of Russian Academy of Sciences, 119334 Moscow, Russia"}],"role":[{"vocabulary":"crossref","role":"author"}]},{"ORCID":"https:\/\/orcid.org\/0000-0003-3361-9136","authenticated-orcid":false,"given":"Nikita G.","family":"Yabbarov","sequence":"additional","affiliation":[{"name":"N. M. 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Emanuel Institute of Biochemical Physics of Russian Academy of Sciences, 119334 Moscow, Russia"}],"role":[{"vocabulary":"crossref","role":"author"}]},{"given":"Dmitry V.","family":"Belykh","sequence":"additional","affiliation":[{"name":"Institute of Chemistry, Komi Scientific Center, Ural Division of the Russian Academy of Sciences, 167982 Syktyvkar, Russia"}],"role":[{"vocabulary":"crossref","role":"author"}]},{"ORCID":"https:\/\/orcid.org\/0000-0002-4411-585X","authenticated-orcid":false,"given":"Olga M.","family":"Startseva","sequence":"additional","affiliation":[{"name":"Pitirim Sorokin Syktyvkar State University, 167001 Syktyvkar, Russia"}],"role":[{"vocabulary":"crossref","role":"author"}]},{"ORCID":"https:\/\/orcid.org\/0000-0001-8259-898X","authenticated-orcid":false,"given":"Anton E.","family":"Egorov","sequence":"additional","affiliation":[{"name":"N. M. 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Semenov Federal Research Center for Chemical Physics of Russian Academy of Sciences, 119991 Moscow, Russia"}],"role":[{"vocabulary":"crossref","role":"author"}]},{"given":"Alexey V.","family":"Krivandin","sequence":"additional","affiliation":[{"name":"N. M. Emanuel Institute of Biochemical Physics of Russian Academy of Sciences, 119334 Moscow, Russia"}],"role":[{"vocabulary":"crossref","role":"author"}]},{"given":"Olga V.","family":"Shatalova","sequence":"additional","affiliation":[{"name":"N. M. Emanuel Institute of Biochemical Physics of Russian Academy of Sciences, 119334 Moscow, Russia"}],"role":[{"vocabulary":"crossref","role":"author"}]},{"ORCID":"https:\/\/orcid.org\/0000-0001-9226-3032","authenticated-orcid":false,"given":"Margarita A.","family":"Gradova","sequence":"additional","affiliation":[{"name":"N. N. 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