Macrophage Targeting pH Responsive Polymersomes for Glucocorticoid Therapy

Pharmaceutics

António Oliveira¹  Alessandro Poma²  Loris Rizzello²  Lorena Ruiz-Perez²  Giuseppe Battaglia²  Salette Reis³  Claudia Nunes³  VirgíniaM. Gouveia³ 

[1] 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;LAQV/REQUIMTE, Department of Chemical Sciences, Faculty of Pharmacy, University of Porto, 4050-313 Porto, Portugal;

关键词: inflammation;    macrophages;    glucocorticoid;    polymersomes;   

DOI  :  10.3390/pharmaceutics11110614

来源: DOAJ

【 摘 要 】

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.

【 授权许可】

Unknown