Amlexanox-loaded nanoliposomes showing enhanced anti-inflammatory activity in cultured macrophages: A potential formulation for treatment of oral aphthous stomatitis

Oral aphthous stomatitis is a common disorder treated with the immunomodulatory drug Amlexanox (AMX), that was administered as mucoadhesive paste (Aphthasol®). This product discontinued by FDA in 2014 due to associated undesired adverse reactions of formulation. Here, we have developed AMX-loaded nanoliposome formulation potential alternative for localised oromucosal delivery AMX. Nanoliposomes were prepared using Soya phosphatidylcholine (SPC) and Cholesterol (Chol) mixtures at three different molar ratios formulate vesicles thin-film hydration, characterised size, zeta entrapment efficiency. The optimal found be SPC:Chol 3:1 efficiency 94%, post sonication. To evaluate anti-inflammatory activity, macrophages differentiation human leukaemia monocytic cell line, THP-1, polarised Interferon gamma (IFNγ) lipopolysaccharide (LPS) M1 state. Macrophages cells D-L1 (SPC:Chol 3:1, 500 μg/mL total lipid, 27.6 μM AMX) showed significant suppression TNF-α expression levels (43 ± 2.7% untreated control, p < 0.05) compared those either empty liposomes or AMX alone. Notably, %TNF-α dramatically decreased 57 4.05% drug-free (500 lipid) indicating activity SPC lipid component per se, which led synergistic effect evident from augmentation Our findings highlight nanoliposomes promising advanced reviving treatment management inflammatory conditions oral mucosa.