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Macrophage Targeting pH Responsive Polymersomes for Glucocorticoid Therapy

2019; Multidisciplinary Digital Publishing Institute; Volume: 11; Issue: 11 Linguagem: Inglês

10.3390/pharmaceutics11110614

1999-4923

Virgínia M. Gouveia, Loris Rizzello, Cláudia Nunes, Alessandro Poma, Lorena Ruiz‐Pérez, António Oliveira, Salette Reis, Giuseppe Battaglia,

RNA Interference and Gene 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.