In vitro biocompatibility study of liposomes differing in (phospho)lipid composition with the keratinocyte cells

Različite vrste liposoma, konvencionalni, deformabilni, propilenglikol i kationski liposomi s uklopljenim azitromicinom, pripremljeni su film metodom. Ekstruzijom kroz polikarbonske membrane, formulacije liposoma su homogenizirane (indeks polidisperznosti < 0,43), a srednji promjeri značajno smanjeni (< 250 nm). Fosfolipidni sastav liposoma imao je utjecaja na površinski naboj liposoma. Konvencionalni, deformabilni i propilenglikol liposomi imali su zeta potencijale od -48 do -44 mV, dok je zeta potencijal kationskih liposoma iznosio + 62 mV. In vitro ispitivanja biokompatibilnosti liposoma s uklopljenim azitromicinom provedena na HaCaT stanicama procijenjena su pomoću MTT testa, mjerenjem metaboličke aktivnosti keratinocita 24 sata nakon inkubacije liposoma s HaCaT stanicama. Uklapanjem u liposome citotoksičnost azitromicina je smanjena. Fosfolipidni sastav i prisustvo suotapala u liposomima su imali utjecaja na biokompatibilnost. Propilenglikol je pokazao povoljan učinak na stanice keratinocita, dok su natrijev deoksikolat i DODAB pokazali potencijalnu citotoksičnost, ali tek pri izuzetno visokim koncentracijama lipida. Imajući u vidu koncentracije azitromicina u liposomima s kojima je postignut odgovarajući antibakterijski učinak, svi ispitivani tipovi liposoma su bili biokompatibilni s HaCaT stanicama.Conventional, deformable, propylene glycol and cationic liposomes encapsulating azithromycin were prepared by the film hydration method. Extrusion of the liposomal dispersions through the polycarbonate membranes resulted with liposomes of more homogenous size distributions with a polydispersity indexes < 0,43 nm and a significantly reduced mean diameters (< 250 nm). The (phospo)lipid composition affected the surface charge of the liposomes. Zeta potential values for the conventional, deformable and propylene glycol liposomes ranged from -48 mV to -44 mV, while the cationic liposomes were shown to have a positive zeta potential of +62 mV. In vitro biocompatibilities of the different types of liposomes containing azithromycin with the human HaCaT cells were evaluated 24 h after the incubation of the cells with the liposomes using the cellular metabolic activity (MTT assay). The encapsulation of azithromycin in liposomes reduced the cytotoxicity of the drug, whereas the (phospo)lipid composition and the presence of the surfactant and cosolvent affected the biocompatibility. Propylene glycol was well tolerated by the keratinocytes in comparison to sodium deoxycholate and DODAB, where potential cytotoxicities were observed. All types of the liposomes were biocompatible with the keratinocytes even at the very high concentrations of azithromycin tested