| Autor: |
Maria Russi, Rachele Valeri, Domenico Marson, Chiara Danielli, Fulvia Felluga, Aura Tintaru, Natasa Skoko, Suzana Aulic, Erik Laurini, Sabrina Pricl |
| Přispěvatelé: |
Russi, Maria, Valeri, Rachele, Marson, Domenico, Danielli, Chiara, Felluga, Fulvia, Tintaru, Aura, Skoko, Natasa, Aulic, Suzana, Laurini, Erik, Pricl, Sabrina |
| Jazyk: |
angličtina |
| Rok vydání: |
2023 |
| Předmět: |
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| Popis: |
Two clinically approved anticancer drugs targeting BRAF in melanoma patients - dabrafenib (DAB) and vemurafenib (VEM) - have been successfully encapsulated into nanomicelles formed upon self-assembly of an amphiphilic dendrimer AD based on two C18 aliphatic chains and a G2 PAMAM head. The process resulted in the formation of well-defined (∼10 nm) core-shell nanomicelles (NMs) with excellent encapsulation efficiency (∼70% for DAB and ∼60% for VEM) and good drug loading capacity (∼27% and ∼24% for DAB and VEM, respectively). Dynamic light scattering (DLS), transmission electron microscopy (TEM), small-angle x-ray scattering (SAXS), nuclear magnetic resonance (NMR), isothermal titration calorimetry (ITC), and molecular simulation (MS) experiments were used, respectively, to determine the size and structure of the empty and drug-loaded nanomicelles (DLNMs), along with the interactions between the NMs and their cargoes. The in vitro release data revealed profiles governed by Fickian diffusion; moreover, for both anticancer molecules, an acidic environment (pH = 5.0) facilitated drug release with respect to physiological pH conditions (pH = 7.4). Finally, both DAB- and VEM-loaded NMs elicited enhanced response with respect to free drug treatments in 4 different melanoma cell lines. |
| Databáze: |
OpenAIRE |
| Externí odkaz: |
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