Impact of formulation parameters on self-assembled liposomes (LeciPlex® III): A detailed investigation

Abstract

The present study investigated the feasibility of fabricating self-assembled liposomes, LeciPlex®, a phospholipid-based vesicular nanocarrier using cationic, anionic, and nonionic stabilizers. The phospholipid investigated was soy phosphatidylcholine and the nano-precipitation method based on solvent diffusion was applied as the fabrication technique of liposomes in this study. The effects of various formulation variables, such as lipid and stabilizer concentration, total solid concentration, and solvent type on the self-assembly of vesicles were studied for physical characterization including particle size analysis, differential scanning calorimetry, viscosity, optical transmittance, transmission electron microscopy, and small angle neutron scattering. All three LeciPlex® systems exhibited a direct relationship between particle size and phospholipid concentration. The two categoric variables, solvent, and stabilizer used to prepare LeciPlex® demonstrated a significant effect on particle size for all three LeciPlex® systems. Small angle neutron scattering, and optical transmittance confirmed the formation of micellar systems at a phospholipid: stabilizer ratio of 1:2 and vesicular systems at a ratio of 2:1 for the systems stabilized with anionic and nonionic surfactants. In contrast to this, the LeciPlex® formed with the cationic stabilizer Dioctadecyldimethylammonium bromide (DODAB), formed vesicles at both ratios. From these investigations, it was clear that the formulation space for LeciPlex® was diversified by the addition of cationic, anionic, and non-ionic stabilizers.

Keywords: Anionic stabilizer; Biocompatible solvents; Cationic stabilizer; LeciPlex®; Liposomes; Non-ionic stabilizer; Physical characterization; Vesicles.