Department of Pharmaceutical Sciences, Faculty of Pharmacy, Universitas Airlangga, Campus C UNAIR, Surabaya, 60115, Indonesia.
Stem Cell Research and Development Center, Universitas Airlangga, Campus C UNAIR, Surabaya, 60115, Indonesia.
Sci Rep. 2023 Mar 15;13(1):4324. doi: 10.1038/s41598-023-31560-5.
β-ionone (ION) is a cyclic terpenoid compound that demonstrates considerable potential for the prevention and treatment of cancer. However, the water solubility of β-ionone is poor and the compound demonstrates low permeability. Liposomes have been reported as increasing both qualities. In this study, the development of β-ionone liposomes was initiated by adding 1,2-dioleoyl-3-trimethylammonium propane (DOTAP) to produce cationic liposomes as a means of enhancing binding to cancer cells. Liposomes composed of β-ionone, HSPC, cholesterol, and DSPE-mPEG were prepared using the thin layer hydration method. Cellular uptake studies were carried out with HeLa cells incubated with β-ionone liposomes for two hours. The results indicated that the addition of DOTAP increased particle size and affected the spectroscopical and thermogram profiles of the liposomes, thereby confirming reduction in liposome crystallinity, while the zeta potential became positive. Moreover, the calcein release profile further showed that additional DOTAP increased both membrane fluidity and cellular uptake in HeLa cells In conclusion, adding DOTAP affected the physicochemical cationic properties of liposome and improved cellular uptake in HeLa cells.
β-紫罗兰酮(ION)是一种环状萜烯化合物,具有很大的预防和治疗癌症的潜力。然而,β-紫罗兰酮的水溶性较差,渗透性也较低。脂质体已被报道可以提高这两种性质。本研究通过添加 1,2-二油酰基-3-三甲铵丙烷(DOTAP)来制备阳离子脂质体,以增强与癌细胞的结合,从而启动了β-紫罗兰酮脂质体的开发。采用薄膜水化法制备了由β-紫罗兰酮、HSPC、胆固醇和 DSPE-mPEG 组成的脂质体。用 HeLa 细胞孵育β-紫罗兰酮脂质体两小时进行细胞摄取研究。结果表明,添加 DOTAP 增加了粒径,并影响了脂质体的光谱和热谱图,从而证实了脂质体结晶度的降低,而zeta 电位变为正。此外,钙黄绿素释放曲线进一步表明,额外添加 DOTAP 增加了 HeLa 细胞的膜流动性和细胞摄取。总之,添加 DOTAP 影响了脂质体的物理化学阳离子性质,并提高了 HeLa 细胞的细胞摄取。