Lipid nanoparticles for topical administration of vitamin D3 and bacterioruberin for the treatment of psoriasis: characterization and in vitro studies

SIMIONI Y.; SCHILRREFF P.; ROMERO E.L; MORILLA M.J

Conferencia; 1st Zooming into preclinical nanomedicines in the era Covid19-.; 2020

Psoriasis, a chronic inflammatory disease, is characterized by overgrowth and abnormal differentiation of keratinocytes, angiogenesis, neutrophil infiltration and increased ROS. Vitamin D3 (VD3) suppresses epidermal proliferation and differentiation. Bacterioruberin (BR) is one of the most effective natural antioxidants. The high hydrophobicity of VD3 and BR and their susceptibility to chemical degradation impair their topical administration. The objective of this work was to combine of BR with VD3 in nanoparticles (VD3-BRNP) to be administered topically. Nanoparticles (NP) made of a core of compritol, BR extract and VD3 covered by a shell of polar archaeolipids from H. tebenquichenseand Tween 80 (2; 2; 1; 1.2; 3% w/w) were prepared by homogenization-ultrasonication. Nanosized (70 ±11 nm), monodisperse (polydispersity index 0.35 ± 0.11), negative Z potential (-38 ± 4 mV), 5 mg/ml VD3 and an inhibitory concentration providing 50% reduction of the DPPH radical (IC50) of 4,8 µg/ml (the activity enhanced by coencapsulation) VD3-BR-NP were obtained. The in vitro release of VD3 was 2 times lower from VD3-BR-NP than control NPs. The release was more gradual. By means of Raman, the characteristic peaks of BR and VD3 were observed. SAXS allowed determining its mesoscopic ordering and lamellarity inalterability when incorporating VD3. An in vitro keratinocyte psoriasis model was developed, and effectiveness of VD3-BR-NP was assessed. VD3-BR-NP, and no control NP (lacking BR), showed anti-inflammatory and antioxidant activity.