Phosphatidylcholine with conjugated linoleic acid in fabrication of novel lipid nanocarriers

Abstract Exploration of novel lipid-based formulations has been an aim for researchers over the last decades. Lipid nanoparticles have been extensively studied as bioactive agent carriers in the pharmaceutical and biomedical fields. In our studies, we have provided properties of two different types of lipid nanocarriers, i.e. solid lipid nanoparticles (SLN) and nanostructured lipid carriers (NLC) prepared via high pressure homogenization. The choice of surfactants in the structural design is one of the most significant approaches to achieve nanocarriers with desirable parameters that acquire both good stability and requested physical state. The present work has been carried out to explore the potential for fabrication of stable and nearly monodisperse lipid nanoparticles stabilized by functionalized phosphatidylcholine, i.e., 1,2-di(conjugated)linoleoyl- sn -glycero-3-phosphocholine ((CLA)PC) which may comprise a potential lipid prodrug. Additionally, 1,2-distearoyl- sn -glycero-3-phosphocholine ((SA)PC) was taken into account as the surfactant to be compared. The sizes of the studied nanosystems (about 130–230 nm in diameter D H ) along with the size distribution (polydiyspersity index PdI below 0.3) were determined by dynamic light scattering (DLS), while the morphology was imaged by atomic force microscopy (AFM). The studied nanoparticles physical state was characterized by differential scanning calorimetry (DSC) and X-ray diffraction (XRD). The NLCs have shown less ordered crystalline structure than the SLNs nanoproducts, this observation being conferred by the inclusion of a liquid lipid. The in vitro cytotoxicity studies were performed on human cancer epidermoid carcinoma (A431) and MeWo cells using trypan blue staining and MTT assays. Nanocarriers labeled by cyanine IR-780 were efficient in bioimaging (MeWo). Our results give new insights into the lipid nanoparticles containing the pharmaceutically promising (CLA)PC and may serve as guidelines for design and preparation of new effective delivery nanosystems, including anti-cancer applications.