Aims: To suppress angiogenesis, auraptene is used in the form of liposome to enhance solubility and effectiveness.

Background: Nanoliposomes are spherical nano-sized capsules enclosed by lipid membranes, serving as a biocompatible vehicle to enhance the delivery of therapeutic agents. Objective: The objective of this research is to prepare and characterize nanoliposome-encapsulated auraptene and compare its cytotoxic and anti-angiogenic effects to non-liposomal auraptene.

Methods: Liposomal auraptene was formulated using DSPC/DSPG/Cholesterol (molar ratio of 4:1:2) in combination with two different molar ratios of auraptene (0.1 and 0.05). The entrapment efficiency was evaluated using High-Performance Liquid Chromatography (HPLC). Various parameters, including Dynamic Light Scattering (DLS), zeta potential, stability, and release kinetics, were investigated. Subsequently, both liposomal and non-liposomal auraptene, along with bare liposomes, were applied to the MDA-MB-231 cell line for a duration of 72 hours at 37°C at varying concentrations. Cytotoxicity was assessed using the MTT assay. Additionally, the study examined the anti-angiogenic effects on the vessels in the chorioallantoic membrane of chick embryos.

Results: The entrapment efficiency of auraptene was found to be satisfactory at 50%. The liposome size ranged from 85 to 241 nm, with a Z-Average of 190.9 nm. The zeta potentials for all formulations were consistently around -55.7, and the Polydispersity Index (PDI) was less than 0.3 for all formulations. The release profile demonstrated approximately 80% drug release over a period of 130 hours. Notably, liposomal auraptene exhibited a significantly lower IC₅₀ value (38.61 [95% Confidence Interval: 30.56 to 48.78]) compared to non-liposomal auraptene (50.36 [95% Confidence Interval: 43.58 to 58.19]) (p = 0.0240). Conclusion: Moreover, the administration of 2.5 and 5 µM of liposomal auraptene led to a reduction in the vessels within the chorioallantoic membrane at the injection site when compared to the control group.

In summary, the use of biodegradable nanoliposomal carriers improved the solubility, release profile, and stability of auraptene while demonstrating anticancer and anti-angiogenic properties.