FIRST STEPS TOWARDS INHALABLE CURCUMIN: CURCUMIN-LOADED NANOARCHAEOSOMES

ALTUBE MARÍA JULIA; LILEN IVONNE CAIMI; MARÍA JOSÉ MORILLA; EDER LILIA ROMERO

Mar del Plata

Conferencia; SAI-SAIC-SAFIS 2018; 2018

Curcumin (CUR) is a hydrophobic polyphenol with antibacterialproperties. However, its low solubility in water hinders its intravenous administration, decreases its oral absorption and systemic bioavailability. In aqueous medium, archaeolipids auto-assemble intonanovesicles called nanoarchaeosomes that, unlike liposomes, remain structurally stable when submitted to nebulization stress. Theincorporation of CUR into ARC would allow the formation of a stable aqueous suspension of CUR, protecting its chemical structureand potentiating its antibacterial activity, thus allowing, for example,its sustained release onto bacterial bioflms located in the lungs.Formulations of CUR loaded in nanoarchaeosomes -AC (archaeolipids:tween80:CUR 1:0.4:0.04 w:w)- and in ordinary liposomes-LC (HSPC:cholesterol:CUR 1:0.33:0.04 w:w)- were prepared bythe lipid flm hydration method and sizes were homogenized bysonication, extrusion and fltration. The AC formulation had a fnallipids:CUR ratio of 1:0.023 w:w whereas LC displayed a lower loading of CUR, of 1:0.003 w:w. The average diameter of AC nanovesicles, measured by dynamic light scattering, was 130 nm, with apolydispersity index (pdi) of 0.22 and a Zeta potential of -18 mV. Forthe LC formulation the size and pdi value were higher: 305 nm and0.84, respectively; and lower Zeta potential of - 4 mV. By evaluating the changes in the absorption spectrum of free CUR vs CUR innanovesicles, it was observed that CUR was nearly eight folds moreextensively partitioned within the lipid bilayer of nanoarchaeosomesthan in liposomes. Furthermore, cytotoxicity of both formulationswas evaluated on the alveolar epithelium cell line A549 to determineranges of safe concentrations for eukaryotic cells. Overall, the ACformulation provided a stable colloidal aqueous suspension of CUR,superior to the one obtained with liposomes in terms of size homogeneity and incorporation effciency, key factors to achieve a successful nebulization of nanovesicles