Objectives:

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

Materials and Methods:

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

Results:

All formulations’ mean sizes were between 134 to 166 nm, and they had a negative charge on their surface. Increasing the cholesteryl hemisuccinate content resulted in a reduction in the size of liposomes. Additionally, all formulations had a low polydispersity index value, which was less than 0.3. All formulations have an EE% of more than 30%. Also, in vitro release of 5-FU from liposome formulations followed the Korsemeyer-Peppas model.

Conclusion:

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

Keywords: 5-Fluorouracil, liposomes, cholesteryl hemisuccinate, small volume incubation method, drug release data modelling