Pharmacological and Diagnostic Research Center, Faculty of Pharmacy, Al-Ahliyya Amman University, Amman, Jordan.
College of Pharmacy, Ras Al Khaimah Medical and Health Sciences University, Ras Al Khaimah, United Arab Emirates.
Sci Prog. 2024 Oct-Dec;107(4):368504241296304. doi: 10.1177/00368504241296304.
This study aimed to repurpose pimozide (PMZ) by incorporating it into nanostructured lipid carriers (NLC) using a modified melting emulsion ultrasonication method.
We employed stearic and oleic acids in a 1:1 ratio as lipids, with Tween 80 and PEG 4000 as surfactants. The formulation was analyzed for particle size, zeta potential, and encapsulation efficiency. Transmission electron microscopy (TEM) was used to confirm the spherical shape of the particles. The release profile of PMZ-NLC was evaluated under different pH conditions, and anticancer activity was tested on A549 cell lines.
The PMZ-NLC exhibited an average particle size of 136 ± 2.9 nm, a zeta potential of -25.1 ± 0.9 mV, and an encapsulation efficiency of 86% ± 11. TEM confirmed the spherical shape of the NLCs. PMZ release from PMZ-NLC was pH-sensitive, enhancing tumor targeting. IC values were 16.5 μM for free PMZ and 12.9 μM for PMZ-NLC after 72 h.
PMZ-NLC demonstrated improved anticancer activity compared to free PMZ, suggesting that encapsulation enhances the drug's effectiveness. The pH-sensitive release profile supports its potential for targeted therapy in lung cancer.
PMZ-NLC showed potential as a safe and effective strategy for lung cancer treatment. Further investigation is warranted to evaluate its in vivo efficacy, long-term safety, and clinical application.
本研究旨在通过将匹莫齐特（PMZ）纳入纳米结构脂质载体（NLC）中，来重新利用 PMZ。方法：我们使用 1:1 比例的硬脂酸和油酸作为脂质，使用吐温 80 和聚乙二醇 4000 作为表面活性剂。对制剂的粒径、Zeta 电位和包封效率进行分析。采用透射电子显微镜（TEM）确认颗粒的球形形状。评估 PMZ-NLC 在不同 pH 条件下的释放情况，并在 A549 细胞系上测试其抗癌活性。结果：PMZ-NLC 表现出平均粒径为 136±2.9nm、Zeta 电位为-25.1±0.9mV 和包封效率为 86%±11%。TEM 证实了 NLC 的球形形状。PMZ-NLC 中的 PMZ 释放具有 pH 敏感性，增强了肿瘤靶向性。72h 后，游离 PMZ 的 IC 值为 16.5μM，PMZ-NLC 的 IC 值为 12.9μM。讨论：与游离 PMZ 相比，PMZ-NLC 表现出增强的抗癌活性，表明包封增强了药物的有效性。pH 敏感性释放特性支持其在肺癌靶向治疗中的潜力。结论：PMZ-NLC 显示出作为治疗肺癌的安全有效策略的潜力。需要进一步研究来评估其体内疗效、长期安全性和临床应用。
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