具有抗癌特性的天然化合物对癌症治疗非常有吸引力。然而，这些化合物的低溶解度和生物利用度限制了它们作为高效抗癌药物的使用。为了避免这些缺点，利用单亚油酸甘油酯和聚氧乙烯辛醇混合物的均质化技术，将这些化合物纳入到立方纳米颗粒（cubosomes）中。从无花果中分离出的天然抗癌化合物茄烯素被用于制备立方纳米颗粒。这些cubosomes的大小、zeta势、包埋效率、小角度X射线衍射、体外释放、体外细胞毒性、细胞吸收和抗肿瘤活性等进行了表征。cubosomes的粒径为220±3.6 nm，zeta势几乎为中性，为-5±1.2 mV，X射线测试证实存在立方结构。此外，超过90%的天然抗癌药物被包埋在cubosomes中。这些cubosomes获得了持续30小时的释放。最后，与自由的天然抗癌化合物相比，这些cubosomes表现出更高的体外细胞毒性和体内肿瘤抑制作用。因此，cubosomes可能是提高该天然化合物抗肿瘤效果的有前途的载体。© 2023 Controlled Release Society。

Natural compounds that elicit anticancer properties are of great interest for cancer therapy. However, the low solubility and bioavailability of these compounds limit their use as efficient anticancer drugs. To avoid these drawbacks, incorporation of these compounds into cubic nanoparticles (cubosomes) was carried out. Cubosomes containing bergapten which is a natural anticancer compound isolated from Ficus carica were prepared by the homogenization technique using monoolein and poloxamer. These cubosomes were characterized for size, zeta potential, entrapment efficiency, small angle X-ray diffraction, in vitro release, in vitro cytotoxicity, cellular uptake, and antitumor activity. Particle size of cubosomes was 220 ± 3.6 nm with almost neutral zeta potential - 5 ± 1.2 mV and X-ray measurements confirmed the existence of the cubic structure. Additionally, more than 90% of the natural anticancer drug was entrapped within the cubosomes. A sustained release over 30 h was obtained for these cubosomes. Finally, these cubosomes illustrated higher in vitro cytotoxicity and in vivo tumor inhibition compared with the free natural anticancer compound. Thus, cubosomes could be promising carriers for enhancement of antitumor efficiency of this natural compound.© 2023. Controlled Release Society.