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Combinatorial Intracellular Delivery Screening of Anticancer Drugs

Sola-Barrado, B; Leite, DM; Scarpa, E; Duro-Castano, A; Battaglia, G; (2020) Combinatorial Intracellular Delivery Screening of Anticancer Drugs. Molecular Pharmaceutics , 17 (12) pp. 4709-4714. 10.1021/acs.molpharmaceut.0c00791. Green open access

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Abstract

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.

Type: Article
Title: Combinatorial Intracellular Delivery Screening of Anticancer Drugs
Open access status: An open access version is available from UCL Discovery
DOI: 10.1021/acs.molpharmaceut.0c00791
Publisher version: http://dx.doi.org/10.1021/acs.molpharmaceut.0c0079...
Language: English
Additional information: This version is the author accepted manuscript. For information on re-use, please refer to the publisher’s terms and conditions.
Keywords: drug screening, combination therapy, polymeric nanoparticles, drug solubilization, intracellular drug delivery, synergy analysis
UCL classification: UCL
UCL > Provost and Vice Provost Offices > UCL BEAMS
UCL > Provost and Vice Provost Offices > UCL BEAMS > Faculty of Maths and Physical Sciences
UCL > Provost and Vice Provost Offices > UCL BEAMS > Faculty of Maths and Physical Sciences > Dept of Chemistry
URI: https://discovery.ucl.ac.uk/id/eprint/10128489
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