Abstract

Thymoquinone (TH), a naturally occurring moiety shows excellent anticancer properties and in the present study, TH loaded polymer hybrid lipid vesicles (TH PLH) were formulated, and in-vitro cytotoxicity towards breast cancer cell lines (MCF-7 and MBD–MB 231 cells) was determined. TH PLH was primed by the ethanol spraying method and were characterized for various attributes like particle size, morphology, percentage drug entrapment, elasticity, rheological, zeta potential, etc. The prepared TH PLH Vesicles showed an average particle size from 344.7 ± 3.7 nm to 351.9 ± 2.3 nm and showed very narrow distribution with polydispersity index ranging from 0.245 ± 0.36 to 0.271 ± 0.66. The surface charge on the vesicles was confirmed by zeta potential (þ −21.3 ± 1.08 mV to þ −19.98 ± 3.4 mV). The globular moulded vesicles were in the nano-size range and had high flexibility and an approximately 10-fold increase in elasticity properties. TH PLH Vesicular gel was formulated by means of Carbopol 934 and was evaluated for physical appearance, pH, rheological behaviour, and skin irritation test. Cytotoxicity study reveals paramount inhibition on cells by TH vesicle-loaded gel. These results showed the high potential of TH PLH vesicles for topical anticancer application.

摘要

百里醌 (TH) 是一种天然存在的部分，显示出优异的抗癌特性，在本研究中，配制了负载 TH 的聚合物杂化脂质囊泡 (TH PLH)，并在体外确定了对乳腺癌细胞系（MCF-7 和 MBD-MB 231 细胞）的细胞毒性。TH PLH 采用乙醇喷涂法引发，并表征了各种属性，如粒径、形态、药物截留百分比、弹性、流变学、zeta 电位等。制备的 TH PLH 囊泡的平均粒径为 344.7 ± 3.7 nm 至351.9 ± 2.3 nm，分布非常窄，多分散指数范围为 0.245 ± 0.36 至 0.271 ± 0.66。通过 zeta 电位（+ -21.3 ± 1.08 mV 至 + -19.98 ± 3.4 mV）确认囊泡上的表面电荷。球状模塑囊泡在纳米尺寸范围内，具有高柔韧性，弹性性能增加约 10 倍。TH PLH 囊泡凝胶通过 Carbopol 934 配制，并评估其物理外观、pH、流变行为和皮肤刺激试验。细胞毒性研究揭示了负载 TH 囊泡的凝胶对细胞的最大抑制作用。这些结果表明 TH PLH 囊泡在局部抗癌应用中具有很高的潜力。