Development and characterization of novel 1-(1-Naphthyl)piperazine-loaded lipid vesicles for prevention of UV-induced skin inflammation

• Published in: European journal of pharmaceutics and biopharmaceutics 2016-07, Vol.104, p.101-109
• Main Authors: Menezes, Ana Catarina, Campos, Patrícia Mazureki, Euletério, Carla, Simões, Sandra, Praça, Fabíola Silva Garcia, Bentley, Maria Vitória Lopes Badra, Ascenso, Andreia
• Format: Article
• Language: English
• Subjects: 1-(1-Naphthyl)piperazine; Animals; Chemoprevention; Cytokines - metabolism; Dermatitis - etiology; In Vitro Techniques; Male; Mice; Mice, Hairless; Peroxidase - metabolism; Piperazines - administration & dosage; Skin cancer; Swine; Topical delivery; Ultradeformable vesicles; Ultraviolet radiation; Ultraviolet Rays; UV-induced acute inflammation
• ISSN: 0939-6411; 1873-3441
• DOI: 10.1016/j.ejpb.2016.04.023

[Display omitted] 1-(1-Naphthyl)piperazine (1-NPZ) has shown promising effects by inhibiting UV radiation-induced immunosuppression. Ultradeformable vesicles are recent advantageous systems capable of improving the (trans)dermal drug delivery. The aim of this study was to investigate 1-NPZ-loaded transethosomes (NPZ-TE) and 1-NPZ-loaded vesicles containing dimethyl sulfoxide (NPZ-DM) as novel delivery nanosystems, and to uncover their chemopreventive effect against UV-induced acute inflammation. Their physicochemical properties were evaluated as follows: vesicles size and zeta potential by dynamic and electrophoretic light scattering, respectively; vesicle deformability by pressure driven transport; rheological behavior by measuring viscosity and I-NPZ entrapment yield by HPLC. In vitro topical delivery studies were performed in order to evaluate the permeation profile of both formulations, whereas in vivo studies sought to assess the photoprotective effect of the selected formulation on irradiated hairless mice by measuring myeloperoxidase activity and the secretion of proinflammatory cytokines. Either NPZ-TE or NPZ-DM exhibited positive results in terms of physicochemical properties. In vitro data revealed an improved permeation of 1-NPZ across pig ear skin, especially by NPZ-DM. In vivo studies demonstrated that NPZ-DM exposure was capable of preventing UVB-induced inflammation and blocking mediators of inflammation in mouse skin. The successful results here obtained encourage us to continue these studies for the management of inflammatory skin conditions that may lead to the development of skin cancers.