Pimozide-loaded nanostructured lipid carriers: Repurposing strategy against lung cancer.

IF 2.6 4区综合性期刊 Q2 MULTIDISCIPLINARY SCIENCES Science Progress Pub Date : 2024-10-01 DOI:10.1177/00368504241296304

Wafa' A Al-Haj, Hamdi Nsairat, Mohamed El-Tanani

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Abstract

Objective: This study aimed to repurpose pimozide (PMZ) by incorporating it into nanostructured lipid carriers (NLC) using a modified melting emulsion ultrasonication method.

Methods: 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.

Results: 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. IC₅₀ values were 16.5 μM for free PMZ and 12.9 μM for PMZ-NLC after 72 h.

Discussion: 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.

Conclusions: 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.

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装载了匹莫齐特的纳米结构脂质载体：针对肺癌的再利用战略

目的：本研究旨在利用改良的熔融乳化超声法，将匹莫齐特（PMZ）加入纳米结构脂质载体（NLC）中，从而实现其再利用：本研究旨在利用改良熔融乳液超声法将匹莫齐特（PMZ）加入纳米结构脂质载体（NLC）中，从而实现其再利用：我们采用硬脂酸和油酸以 1:1 的比例作为脂质，Tween 80 和 PEG 4000 作为表面活性剂。对配方的粒度、ZETA电位和封装效率进行了分析。透射电子显微镜（TEM）确认了颗粒的球形。评估了 PMZ-NLC 在不同 pH 值条件下的释放曲线，并对 A549 细胞系进行了抗癌活性测试：结果：PMZ-NLC的平均粒径为136 ± 2.9 nm，zeta电位为-25.1 ± 0.9 mV，封装效率为86% ± 11。TEM确认了NLC的球形。PMZ-NLC的PMZ释放对pH值敏感，从而增强了肿瘤靶向性。72小时后，游离PMZ的IC50值为16.5 μM，而PMZ-NLC的IC50值为12.9 μM：讨论：与游离 PMZ 相比，PMZ-NLC 的抗癌活性有所提高，这表明封装可增强药物的有效性。对 pH 值敏感的释放特征支持了其用于肺癌靶向治疗的潜力：PMZ-NLC显示出作为一种安全有效的肺癌治疗策略的潜力。结论：PMZ-NLC作为一种安全有效的肺癌治疗策略具有潜力，但还需要进一步研究，以评估其体内疗效、长期安全性和临床应用。

本文章由计算机程序翻译，如有差异，请以英文原文为准。

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来源期刊

Science Progress Multidisciplinary-Multidisciplinary

CiteScore

3.80

自引率

0.00%

发文量

119

期刊介绍： Science Progress has for over 100 years been a highly regarded review publication in science, technology and medicine. Its objective is to excite the readers'' interest in areas with which they may not be fully familiar but which could facilitate their interest, or even activity, in a cognate field.