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Macrophage Targeting pH Responsive Polymersomes for Glucocorticoid Therapy

LAQV/REQUIMTE, Department of Chemical Sciences, Faculty of Pharmacy, University of Porto, 4050-313 Porto, Portugal
Abel Salazar Biomedical Sciences Institute, University of Porto, Portugal, 4050-313 Porto, Portugal
Department of Chemistry, University College London, 20 Gordon Street, London WC1H 0AJ, UK
Institute of Physics of Living Systems, University College London, 20 Gordon Street, London WC1H 0AJ, UK
Institute for Bioengineering of Catalonia (IBEC), The Barcelona Institute of Science and Technology, Baldiri Reixac 10-12, 08028 Barcelona, Spain
Division of Biomaterials and Tissue Engineering, UCL Eastman Dental Institute, University College London, 256 Gray’s Inn Road, London WC1X 8LD, UK
EPSRC/JEOL Centre for Liquid Phase Electron Microscopy, University College London, 20 Gordon Street, London WC1H 0AJ, UK
Catalan Institution for Research and Advanced Studies (ICREA), Passeig Lluís Companys 23, 08010 Barcelona, Spain
Authors to whom correspondence should be addressed.
Pharmaceutics 2019, 11(11), 614;
Received: 9 October 2019 / Revised: 11 November 2019 / Accepted: 12 November 2019 / Published: 15 November 2019
(This article belongs to the Special Issue Emerging Micro- and Nanofabrication Technologies for Drug Delivery)
Glucocorticoid (GC) drugs are the cornerstone therapy used in the treatment of inflammatory diseases. Here, we report pH responsive poly(2-methacryloyloxyethyl phosphorylcholine)–poly(2-(diisopropylamino)ethyl methacrylate) (PMPC–PDPA) polymersomes as a suitable nanoscopic carrier to precisely and controllably deliver GCs within inflamed target cells. The in vitro cellular studies revealed that polymersomes ensure the stability, selectivity and bioavailability of the loaded drug within macrophages. At molecular level, we tested key inflammation-related markers, such as the nuclear factor-κB, tumour necrosis factor-α, interleukin-1β, and interleukin-6. With this, we demonstrated that pH responsive polymersomes are able to enhance the anti-inflammatory effect of loaded GC drug. Overall, we prove the potential of PMPC–PDPA polymersomes to efficiently promote the inflammation shutdown, while reducing the well-known therapeutic limitations in GC-based therapy. View Full-Text
Keywords: inflammation; macrophages; glucocorticoid; polymersomes inflammation; macrophages; glucocorticoid; polymersomes
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MDPI and ACS Style

Gouveia, V.M.; Rizzello, L.; Nunes, C.; Poma, A.; Ruiz-Perez, L.; Oliveira, A.; Reis, S.; Battaglia, G. Macrophage Targeting pH Responsive Polymersomes for Glucocorticoid Therapy. Pharmaceutics 2019, 11, 614.

AMA Style

Gouveia VM, Rizzello L, Nunes C, Poma A, Ruiz-Perez L, Oliveira A, Reis S, Battaglia G. Macrophage Targeting pH Responsive Polymersomes for Glucocorticoid Therapy. Pharmaceutics. 2019; 11(11):614.

Chicago/Turabian Style

Gouveia, Virgínia M.; Rizzello, Loris; Nunes, Claudia; Poma, Alessandro; Ruiz-Perez, Lorena; Oliveira, António; Reis, Salette; Battaglia, Giuseppe. 2019. "Macrophage Targeting pH Responsive Polymersomes for Glucocorticoid Therapy" Pharmaceutics 11, no. 11: 614.

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