提高载药磷脂酰肌醇制剂中扁柏酚对乳腺癌细胞系的细胞毒性活性。
Improving the Cytotoxic Activity of Hinokitiol from Drug-Loaded Phytosomal Formulation Against Breast Cancer Cell Lines.
发表日期:2024
作者:
Tarek A Ahmed, Ghada A Milibary, Alshaimaa M Almehmady, Amerh A Alahmadi, Ehab M M Ali, Khalid M El-Say
来源:
International Journal of Nanomedicine
摘要:
本研究调查了各种配方参数对负载扁柏酚的磷脂质体特性的影响,并评估了其对乳腺癌细胞的抗癌潜力。制备了磷脂质体纳米颗粒,并对其尺寸、zeta 电位和包封效率进行了表征。使用光学显微镜和透射电子显微镜(TEM)进行形态分析。测定了扁柏酚在不同 pH 水平下的溶解度,并评估了优化的磷脂复合物的体外释放曲线。进行细胞毒性测定以评估对乳腺癌细胞系的抗癌功效,并使用膜联蛋白 V/碘化丙啶染色检查细胞凋亡诱导。进行细胞周期分析以评估对细胞周期进展的影响。优化的磷脂酶的尺寸范围为 138.4 ± 7.7 至 763.7 ± 15.4 nm,zeta 电位范围为 -10.2 ± 0.28 至 -53.2 ± 1.06 mV,包封效率介于29.161±1.163%和92.77±7.01%。形态表征证实了均匀性和球形形态。扁柏酚的溶解度随着 pH 值的增加而增加,并且从优化的磷脂体中的释放表现出持续的模式。与纯桧醇相比,配制的磷脂复合物显示出优异的细胞毒性,IC50 值更低。治疗诱导显着的细胞凋亡和细胞周期停滞在 G2/M 和 S 期。负载扁柏酚的植物体表现出对乳腺癌细胞有前景的抗癌功效,突出了它们作为乳腺癌治疗靶向治疗剂的潜力。© 2024 Ahmed 等人。
This study investigates the influence of various formulation parameters on the characteristics of hinokitiol-loaded phytosomes and evaluates their anticancer potential against breast cancer cells.Phytosomal nanoparticles were prepared and characterized for size, zeta potential, and entrapment efficiency. Morphological analysis was conducted using optical microscopy and transmission electron microscopy (TEM). The solubility of hinokitiol at different pH levels was determined, and the in vitro release profile of the optimized phytosomes was assessed. Cytotoxicity assays were performed to evaluate the anticancer efficacy against breast cancer cell lines, and apoptosis induction was examined using Annexin V/propidium iodide staining. Cell cycle analysis was conducted to assess the impact on cell cycle progression.The optimized phytosomes demonstrated a size range of 138.4 ± 7.7 to 763.7 ± 15.4 nm, with zeta potentials ranging from -10.2 ± 0.28 to -53.2 ± 1.06 mV and entrapment efficiencies between 29.161 ± 1.163% and 92.77 ± 7.01%. Morphological characterization confirmed uniformity and spherical morphology. Hinokitiol solubility increased with pH, and the release from the optimized phytosomes exhibited sustained patterns. The formulated phytosomes showed superior cytotoxicity, with lower IC50 values compared to pure hinokitiol. Treatment induced significant apoptosis and cell cycle arrest at the G2/M and S phases.Hinokitiol-loaded phytosomes demonstrate promising anticancer efficacy against breast cancer cells, highlighting their potential as targeted therapeutic agents for breast cancer therapy.© 2024 Ahmed et al.