This research highlights the capacity of a newly introduced centrifugation process to form liposomes from water-in-fluorocarbon nano-emulsions stabilized with phospholipids to incorporate macromolecular and sensitive active pharmaceutical ingredients (API). The encapsulation efficiency of the produced liposomes, incorporating fluorescein-sodium, bovine serum albumin and fluorecein isothiocyanate dextran as model APIs, is determined by applying Vivaspin® centrifugation filtration and quantified by UV-Vis spectroscopy. It was found that higher densities of the fluorocarbons used as the hydrophobic phase enable a higher encapsulation efficiency and that an efficiency of up to 98% is possible depending on the used phospholipid. Among the engineering aspects of the process, a comparison between different membrane substances was performed. Efficiency increases with a higher phospholipid concentration but decreases with the addition of cholesterol. Due to the higher bending modulus, liposome formation is slowed down by cholesterol during liposome closure leading to a greater leakage of the model API. The encapsulation of bovine serum albumin and dextran, both investigated under different osmotic conditions, shows that an efflux negatively affects the encapsulation efficiency while an influx increases the stability. Overall, the process shows the potential for a very high encapsulation efficiency for macromolecules and future pharmaceutical applications.
Fluorocarbons are one of the most promising hydrophobic phases for future pharmaceutical production processes and various biomedical applications. Yet, because of their specific characteristics such as high density and refractive index similar to water, analysis of water‐in‐fluorocarbon (w/fc) nanoemulsions remains a challenge. The present work examines w/fc nanoemulsions stabilized with phospholipids as natural emulsifiers and tackles the measuring problems of photon correlation spectroscopy (PCS) when used for investigation of fluorocarbon nanoemulsions. These emulsions are suitable to form liposomes via centrifugation and thus, are required to meet certain criteria such as stability and size. The results imply a stability of up to 4 weeks with an average size of 180 nm. The intensity mean diameter gained from PCS measurements shows large scattering directly after sonication which is due to gas bubbles from sonication. The number mean is not influenced by gas bubbles and gives a more accurate depiction of the produced nanoemulsions. These findings are supported by small‐angle X‐ray scattering data, which are additionally applied for liposome analysis measuring a size of approximately 60 nm.