Stearyl amine tailored spanlastics embedded within tetronic^® nanogel for boosting the repurposed anticancer potential of mebendazole: formulation, in vitro profiling, cytotoxicity assessment, and in vivo permeation analysis.

IF 2.5 4区医学 Q3 PHARMACOLOGY & PHARMACY

DARU Journal of Pharmaceutical Sciences Pub Date : 2025-03-29 DOI:10.1007/s40199-025-00560-3

Mai El Halawany, Marwa Sharaky, Diana Aziz

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Abstract

Background: Mebendazole (MBZ) is an anthelmintic drug that was repurposed as an anti-cancer agent.

Objectives: This study aimed at formulating MBZ into stearylamine tailored spanlastics dispersed in nanogel for enhancing MBZ anti-tumor efficacy against skin cancer.

Methods: MBZ spanlastics were prepared by thin film hydration using 2¹ × 3¹ factorial design. The formulation variables were the total amount (mg) of Span 60 and Tween 80 in the formulations and the ratio between Span 60 and Tween 80.

Results: Optimal spanlastics formulation was composed of 400 mg of Span 60 and Tween 80 in a ratio of 2:1 and showed EE% of 78 ± 2.9% and PS of 284.00 ± 35.36 nm. Stearylamine (20 mg) was added to the optimized formulation and showed acceptable positive charge (zeta potential = 47.53 ± 1.50 mV). It was dispersed in 30% Tetronic^®1107 solution to form a nanogel. MBZ nanogel was assessed for their cytotoxic effect on cell proliferation against human malignant melanoma and epidermoid carcinoma cell lines and showed 38.70 ± 1.70% and 48.60 ± 0.50% (respectively) cell proliferation compared to the control group (100%). Finally, its permeation through Wistar rat skin was tested.

Conclusion: SA-spanlastics nanogel holds potential as an effective nanocarrier for boosting MBZ anti-cancer efficacy.

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硬脂酰胺量身定制的塑料嵌入到tetronic®纳米凝胶中，以提高甲苯达唑的抗癌潜力：配方，体外分析，细胞毒性评估和体内渗透分析。

背景：甲苯达唑（MBZ）是一种驱虫药，被重新用作抗癌药物。目的：本研究旨在将MBZ制成分散在纳米凝胶中的硬脂胺定制塑料，以增强MBZ对皮肤癌的抗肿瘤作用。方法：采用21 × 31析因设计，采用薄膜水化法制备MBZ塑料。配方变量为Span 60和Tween 80在配方中的总用量（mg）和Span 60与Tween 80的比值。结果：最佳配方为Span 60与Tween 80以2:1的比例组合400 mg，其EE%为78±2.9%，PS为284.00±35.36 nm。优化后的配方中加入硬脂胺（20 mg），正电荷可接受（zeta电位= 47.53±1.50 mV）。将其分散在30%的Tetronic®1107溶液中形成纳米凝胶。MBZ纳米凝胶对人恶性黑色素瘤和表皮样癌细胞增殖的细胞毒作用，与对照组（100%）相比，细胞增殖率分别为38.70±1.70%和48.60±0.50%。最后，测试其在Wistar大鼠皮肤中的渗透性。结论：sa -弹塑性纳米凝胶作为一种有效的纳米载体，具有提高MBZ抗癌效果的潜力。

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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DARU Journal of Pharmaceutical Sciences PHARMACOLOGY & PHARMACY-

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期刊介绍： DARU Journal of Pharmaceutical Sciences is a peer-reviewed journal published on behalf of Tehran University of Medical Sciences. The journal encompasses all fields of the pharmaceutical sciences and presents timely research on all areas of drug conception, design, manufacture, classification and assessment. The term DARU is derived from the Persian name meaning drug or medicine. This journal is a unique platform to improve the knowledge of researchers and scientists by publishing novel articles including basic and clinical investigations from members of the global scientific community in the forms of original articles, systematic or narrative reviews, meta-analyses, letters, and short communications.