Influence of Formulation Composition on the Characteristic Properties of 5-fluorouracil-loaded Liposomes

Variations in the types and quantities of excipients used to prepare liposomes can affect the physicochemical properties of liposome formulations. This study aimed to provide information about the design and fabrication of 5-fluorouracil (5-FU)-loaded liposome formulations using different lipid and cholesterol (CHOL) derivatives.

Passive loading via a small-volume incubation method was used to prepare liposomes. The particle size, polydispersity index, zeta potential, and encapsulation efficiency (EE%) of the formulations were determined. The release studies of the formulations were conducted using a Franz diffusion cell at 37 °C. In this study, a high-pressure liquid chromatography device was used to measure the amount of 5-FU.

The mean particle sizes of all formulations were between 134 and 166 nm, and they had a negative charge on their surface. Increasing the cholesteryl hemisuccinate content reduced the size of the liposomes. Additionally, all formulations exhibited a low polydispersity index (0.3). The EE% of all formulations exceeded 30%. The in vitro release of 5-FU from liposome formulations followed the Korsemeyer-Peppas model.

Modifying the lipid and CHOL content in the formulations, as indicated by the experimental results, can change the characteristic properties of liposomes. The use of soybean phosphatidylcholine and cholesteryl hemisuccinate appears to be a promising combination for the preparation of hydrophilic drug-loaded liposome formulations.