Erythrocyte-derived liposomes for the treatment of inflammatory diseases

Abstract

Effective and safe therapies to counteract persistent inflammation are necessary. We developed erythrocyte-derived liposomes (EDLs) with intrinsic anti-inflammatory activity. The EDLs were prepared using lipids extracted from erythrocyte membranes, which are rich in omega-3 fatty acids with several health benefits. Diclofenac, a widely used anti-inflammatory drug, was incorporated into EDLs in relevant therapeutic concentrations. The EDLs were also functionalised with folic acid to allow their active targeting of M1 macrophages, which are key players in inflammatory processes. In the presence of lipopolysaccharide (LPS)-stimulated macrophages, empty EDLs and EDLs incorporating diclofenac were able to reduce the levels of important pro-inflammatory cytokines, namely interleukin-6 (IL-6; ≈85% and 77%, respectively) and tumour necrosis factor-alpha (TNF-α; ≈64% and 72%, respectively). Strikingly, cytocompatible concentrations of EDLs presented similar effects to dexamethasone, a potent anti-inflammatory drug, in reducing IL-6 and TNF-α concentrations, demonstrating the EDLs potential to be used as bioactive carriers in the treatment of inflammatory diseases.

Keywords:

• Erythrocytes
• inflammatory diseases
• liposomes
• active targeting
• drug delivery
• anti-inflammatory activity

Disclosure statement

No potential conflict of interest was reported by the author(s).

Additional information

Funding

Authors acknowledge the financial support from the Fundação para a Ciência e a Tecnologia (FCT) to the PhD grant PD/BD/135246/2017, CEECIND/03628/2017 and CEECIND/04058/2018 and the project Cells4_IDs (PTDC/BTM-SAL/28882/2017), and the NORTE 2020 Structured Project, cofunded by Norte2020 (NORTE-01-0145-FEDER-000021). The authors would also like to acknowledge the additional support provided by FCT (UIDB/50026/2020 and UIDP/50026/2020). Authors would also like to thank CEF-Taipas for the blood donations.