Improved Therapeutic Efficacy: Liposome-Coated Mesoporous Silica Nanoparticles Delivering Thymoquinone to MCF-7 Cells.

Pooria M Arvejeh, Fatemeh A Chermahini, Amin Soltani, Zahra Lorigooini, Mahmoud Rafieian-Kopaei, Gholam Reza Mobini, Pegah Khosravian
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Abstract

Background: Breast cancer remains a significant global health challenge, with thymoquinone showing promise as a therapeutic agent, but hindered by poor solubility.

Objective: This study aimed to enhance TQ delivery to MCF-7 breast cancer cells using mesitylene- mesoporous silica nanoparticles coated with liposomes, designed for controlled drug release.

Methods: Nanoparticles were synthesized using the sol-gel method and coated with phosphatidylserine- cholesterol liposomes. Different nanocharacterization techniques and in vitro assays were employed to assess the drug release kinetics, cellular uptake, cytotoxicity, and apoptosis.

Results: The nanoparticles exhibited favorable properties, including a large pore size of 3.6 nm, a surface area of 248.96 m2/g, and a hydrodynamic size of 171.571 ± 8.342 nm with a polydispersity index of 0.182 ± 0.017, indicating uniformity and stability. The successful lipid bilayer coating was confirmed by a zeta potential shift from +6.25 mV to -5.65 mV. The coated nanoparticles demonstrated a slow and sustained drug release profile, with cellular uptake of FITC-formulated nanoparticles being approximately 5-fold higher than free FITC (P < 0.0001). Cytotoxicity assays revealed a significant reduction in cell viability (P < 0.0001), reaching an IC50 value of 25 μM at 48 hours. Apoptosis rates were significantly higher in cells treated with the formulated TQ compared to the free drug and control at both 24 and 48 hours (P < 0.0001).

Conclusion: This nanoformulation significantly enhanced TQ delivery, offering a promising strategy for targeted breast cancer therapy. Further preclinical studies are recommended to advance this approach in cancer treatment.

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提高疗效:向 MCF-7 细胞输送胸腺醌的脂质体包裹介孔二氧化硅纳米粒子。
背景:乳腺癌仍然是全球健康的重大挑战:胸腺醌有望成为一种治疗药物,但其溶解性较差:本研究旨在使用涂有脂质体的间苯二酚-间孔二氧化硅纳米粒子,加强对 MCF-7 乳腺癌细胞的胸腺喹酮给药:方法:采用溶胶-凝胶法合成纳米颗粒,并包覆磷脂酰丝氨酸-胆固醇脂质体。采用不同的纳米表征技术和体外试验来评估药物释放动力学、细胞吸收、细胞毒性和细胞凋亡:结果:纳米颗粒表现出良好的特性,包括大孔径(3.6 nm)、比表面积(248.96 m2/g)、水动力粒径(171.571 ± 8.342 nm)和多分散指数(0.182 ± 0.017),表明其均匀性和稳定性。ZETA 电位从 +6.25 mV 变为 -5.65 mV,证实了脂质双分子层包覆的成功。包覆的纳米颗粒表现出缓慢而持续的药物释放特性,细胞对 FITC 配制纳米颗粒的吸收率比游离 FITC 高出约 5 倍(P < 0.0001)。细胞毒性试验显示,细胞活力显著降低(P < 0.0001),48 小时后的 IC50 值达到 25 μM。与游离药物和对照组相比,用配制的 TQ 处理的细胞在 24 小时和 48 小时内的凋亡率明显更高(P < 0.0001):结论:这种纳米制剂能明显增强 TQ 的递送,为乳腺癌靶向治疗提供了一种前景广阔的策略。建议进一步开展临床前研究,以推进这种方法在癌症治疗中的应用。
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