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Combinatorial Intracellular Delivery Screening of Anticancer Drugs

  • Belen Sola-Barrado
    Belen Sola-Barrado
    Department of Chemistry, University College London, London WC1H 0AJ, United Kingdom
    Institute for the Physics of Living Systems, University College London, London WC1E 6BT, United Kingdom
  • Diana M. Leite
    Diana M. Leite
    Department of Chemistry, University College London, London WC1H 0AJ, United Kingdom
    Institute for the Physics of Living Systems, University College London, London WC1E 6BT, United Kingdom
  • Edoardo Scarpa
    Edoardo Scarpa
    Department of Chemistry, University College London, London WC1H 0AJ, United Kingdom
    Institute for the Physics of Living Systems, University College London, London WC1E 6BT, United Kingdom
  • Aroa Duro-Castano
    Aroa Duro-Castano
    Department of Chemistry, University College London, London WC1H 0AJ, United Kingdom
    Institute for the Physics of Living Systems, University College London, London WC1E 6BT, United Kingdom
  • , and 
  • Giuseppe Battaglia*
    Giuseppe Battaglia
    Department of Chemistry, University College London, London WC1H 0AJ, United Kingdom
    Institute for the Physics of Living Systems, University College London, London WC1E 6BT, United Kingdom
    Institute for Bioengineering of Catalonia (IBEC), The Barcelona Institute for Science and Technology (BIST), Barcelona 08036, Spain
    Catalan Institution for Research and Advanced Studies (ICREA), Barcelona 08010, Spain
    *Email: [email protected]
Cite this: Mol. Pharmaceutics 2020, 17, 12, 4709–4714
Publication Date (Web):November 11, 2020
https://doi.org/10.1021/acs.molpharmaceut.0c00791
Copyright © 2020 American Chemical Society

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    Abstract

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    Conventional drug solubilization strategies limit the understanding of the full potential of poorly water-soluble drugs during drug screening. Here, we propose a screening approach in which poorly water-soluble drugs are entrapped in poly(2-(methacryloyloxyethyl phosphorylcholine)-poly(2-(diisopropylaminoethyl methacryate) (PMPC–PDPA) polymersomes (POs) to enhance drug solubility and facilitate intracellular delivery. By using a human pediatric glioma cell model, we demonstrated that PMPC–PDPA POs mediated intracellular delivery of cytotoxic and epigenetic drugs by receptor-mediated endocytosis. Additionally, when delivered in combination, drug-loaded PMPC–PDPA POs triggered both an enhanced drug efficacy and synergy compared to that of a conventional combinatorial screening. Hence, our comprehensive synergy analysis illustrates that our screening methodology, in which PMPC–PDPA POs are used for intracellular codelivery of drugs, allows us to identify potent synergistic profiles of anticancer drugs.

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    The Supporting Information is available free of charge at https://pubs.acs.org/doi/10.1021/acs.molpharmaceut.0c00791.

    • Morphology of PMPC–PDPA POs, characterization of PTX-, CRF-, and PNB-loaded PMPC–PDPA POs, characterization of PMPC–PDPA POs by DLS, PMPC–PDPA POs uptake by glioma cells, PMPC–PDPA POs uptake by F98 cells at 24 h of incubation, dose–response curves of cell viability of SF8628 cells treated with either free PNB, PTX, or CRF dissolved in DMSO and PNB–POs, PTX–POs, or CRF-POs over 24 h of incubation and different drug doses, and drug synergy analysis (PDF)

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    Cited By

    This article is cited by 8 publications.

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    2. Kensuke Yoshie, Kazuhiko Ishihara. Solubilization of Poorly Water-soluble Drugs with Amphiphilic Phospholipid Polymers. YAKUGAKU ZASSHI 2023, 143 (9) , 745-756. https://doi.org/10.1248/yakushi.23-00023
    3. Safa Almadhi, Joe Forth, Laura Rodriguez‐Arco, Aroa Duro‐Castano, Ian Williams, Lorena Ruiz‐Pérez, Giuseppe Battaglia. Bottom‐Up Preparation of Phase‐Separated Polymersomes. Macromolecular Bioscience 2023, 23 (8) https://doi.org/10.1002/mabi.202300068
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