Electroformation of Particulate Emulsions Using Lamellar and Nonlamellar Lipid Self-Assemblies.

We report on the development of an electroformation technique for the preparation of particulate (particle-based) emulsions. These oil-in-water (here, lipid phase acts as an "oil") emulsions were prepared using nonlamellar lipid phases. Such emulsion particles offer high hydrophobic volumes compared to conventional lipid particles based on lamellar phases (vesicles/liposomes). In addition, the tortuous internal nanostructure contributes through greater surface area per volume of lipid particles allowing an enhanced loading of payloads. The electroformation method makes use of a capacitor formed from two indium tin oxide coated conductive glass surfaces separated by a dielectric aqueous medium. This capacitor setup is enclosed in a custom-designed 3D-printed unit. Lipid molecules, deposited on conductive surfaces, self-assemble into a nanostructure in the presence of an aqueous medium, which when subjected to an alternating current electric field forms nano- and/or microparticles. Optical microscopy, dynamic light scattering, and small-angle X-ray scattering techniques were employed for micro- and nanostructural analyses of electroformed particles. With this method, it is possible to produce particulate emulsions at a very low (e.g., 0.0005 wt % or 0.5 mg/mL) lipid concentration. We demonstrate an applicability of the electroformation method for drug delivery by preparing lipid particles with curcumin, which is a highly important but water-insoluble medicinal compound. As the method employs gentle conditions, it is potentially noninvasive for the delivery of delicate biomolecules and certain drugs, which are prone to decomposition or denaturation due to the high thermomechanical energy input and/or nonaqueous solvents required for existing methods.

Self-Assembled Lipid Cubic Phase and Cubosomes for the Delivery of Aspirin as a Model Drug.

Three-dimensionally organized lipid cubic self-assemblies and derived oil-in-water emulsions called "cubosomes" are attractive for various biotechnological applications due to their ability to be loaded with functional molecules and their associated sustained release properties. Here, we employed both of these lipid-based systems for the delivery of a model drug, aspirin, under comparable conditions. Studies were performed by varying drug-to-lipid ratio and the type of release medium, water and phosphate buffer saline (PBS). Release rates were determined using UV-vis spectroscopy, and small-angle X-ray scattering was used to confirm the type of self-assembled nanostructures formed in these lipid systems. The release from the bulk lipid cubic phase was sustained as compared to that of dispersed cubosomes, and the release in PBS was more efficient than in water. The tortuosity of the architecture, length of the diffusion pathway, type of nanostructure, and physicochemical interaction with the release media evidently contribute to these observations. This work is particularly important as it is the first report where both of these nanostructured lipid systems have been studied together under similar conditions. This work provides important insights into understanding and therefore controlling the release behavior of lipid-based drug nanocarriers.