Colloidal formulations of etoposide based on self-assembling oleyl-hyaluronan-based structures: optimization of technology and in vitro analysis

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dc.authorscopusidAlexander S. Novikov / 50262902200
dc.authorwosidAlexander S. Novikov / L-5001-2015
dc.contributor.authorAntonova, M.M.
dc.contributor.authorKarshieva, S.Sh.
dc.contributor.authorNikitin, A.A.
dc.contributor.authorMalinovskaya, Yu.A.
dc.contributor.authorErmolin, D.V.
dc.contributor.authorNovikov, Alexander S.
dc.contributor.authorSkorb, E.V.
dc.contributor.authorBeigulenko, D.V.
dc.contributor.authorKovshova, T.S.
dc.contributor.authorKalacheva, E.A.
dc.contributor.authorFilin, A.A.
dc.contributor.authorGelperina, S.E.
dc.date.accessioned2025-04-17T10:11:10Z
dc.date.available2025-04-17T10:11:10Z
dc.date.issued2025
dc.departmentİstinye Üniversitesi, Mühendislik ve Doğa Bilimleri Fakültesi, Kimya Bölümü
dc.description.abstractThe ability of the conjugate of hyaluronic acid and oleic acid (oleyl hyaluronan — HA-C18:1) to form self-assembling micellar structures was utilized to enhance the water solubility of the anticancer drug etoposide (ETP) and its prodrug, 4-O′-benzyloxycarbonyl derivative (ETP-Cbz). Using density functional theory (DFT), it was established that the ETP-Cbz associate with HA-C18:1 had greater thermodynamic stability compared to the ETP associate, which was confirmed experimentally. The micelles loaded with ETP-Cbz were smaller (268 nm compared to 407 nm), more stable (with the critical micelle concentration (CMC) decreasing from 0.07 to 0.025 mg/mL), and had the higher drug loading efficiency (82 %) as compared to HA-C18:1/ETP micelles. In vitro experiments showed that both micellar formulations exhibited low hemolytic activity and delayed drug release profiles during the first hours. In vitro cytotoxicity against MCF-7 and MDA-MB-231 cell lines showed the dose-dependent decrease in cell viability whereas the toxic effect against normal human dermal fibroblasts (NHDF) was significantly lower and exceeded the concentration of HA-C18:1 in the micellar formulations. Confocal microscopy was used to confirm the active uptake of micellar formulations by MDA-MB-231 cells. These findings, therefore, suggest that HA-C18:1 may be a promising solubilizing agent for etoposide and its prodrug.
dc.description.sponsorshipNational Research Council Canada Russian Science Foundation Russian Science Foundation
dc.identifier.citationAntonova, M. M., Karshieva, S. S., Nikitin, A. A., Malinovskaya, Y. A., Ermolin, D. V., Novikov, A. S., ... & Ermolenko, Y. V. (2025). Colloidal formulations of etoposide based on self-assembling oleyl-hyaluronan-based structures: Optimization of technology and in vitro analysis. Nano-Structures & Nano-Objects, 41, 101443.
dc.identifier.doi10.1016/j.nanoso.2025.101443
dc.identifier.endpage11
dc.identifier.issn2352507X
dc.identifier.scopus2-s2.0-85216334800
dc.identifier.scopusqualityQ1
dc.identifier.startpage1
dc.identifier.urihttp://dx.doi.org/10.1016/j.nanoso.2025.101443
dc.identifier.urihttps://hdl.handle.net/20.500.12713/6183
dc.identifier.volume41
dc.indekslendigikaynakScopus
dc.institutionauthorNovikov, Alexander S.
dc.institutionauthoridAlexander S. Novikov / 0000-0001-9913-5324
dc.language.isoen
dc.publisherElsevier b.v.
dc.relation.ispartofNano-structures and nano-objects
dc.relation.publicationcategoryMakale - Uluslararası Hakemli Dergi - Kurum Öğretim Elemanı
dc.rightsinfo:eu-repo/semantics/closedAccess
dc.subjectEtoposide
dc.subjectEtoposide Prodrug
dc.subjectHyaluronic Acid
dc.subjectHydrophobized Hyaluronic Acid
dc.subjectMicellar Forms
dc.titleColloidal formulations of etoposide based on self-assembling oleyl-hyaluronan-based structures: optimization of technology and in vitro analysis
dc.typeArticle

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