Introduction

Cervical cancer is one of the most common cancers among women, and its mortality rate is increasing rapidly. Drugs such as paclitaxel are used to treat this cancer. Unfortunately, the hydrophobic nature of this drug increases its side effects. Polymeric micro-rods are suitable carriers that can be used to transport hydrophobic drugs such as paclitaxel and release the drug in a slow and controlled manner. The aim of this study is to load paclitaxel onto polymeric inulin stearate micro-rods and evaluate these rods for physicochemical properties, drug release, and cytotoxicity.

Materials and Methods

Inulin was reacted with stearoyl chloride in the presence of 4-dimethylaminopyridine until the inulin stearate was made and lyophilized after purification. Using dialysis method, paclitaxel was loaded onto polymeric micro-rods with two final formulations of 10 and 20%. The prepared rods were studied for surface charge, morphology, loading efficiency, drug release, and the effects of cytotoxicity on HeLa cell line.

Results

In water solvent and by dialysis method, inulin stearate interacts with paclitaxel and produces micro-rod with self-assembly approach. SEM images prove the structure of micro-rods. The surface charge of 10% and 20% rods were − 8.19 and − 10.5 mV, respectively. Percentage of drug loading for 10% was 6.33% and for 20% was 14.89%. Finally, evaluation of in vitro drug release showed a sustained and slow release of the drug. Analysis of drug release charts for the two formulations showed that 20% formulation is more suitable for slow drug release studies than 10%. Cytotoxicity results for the 20% formulation also showed that the IC₅₀ value for drug-loaded inulin stearate rods on the HeLa cell line was 3.1 μM.

Conclusion

In this study, inulin stearate rods containing paclitaxel (20%) exhibited good in vitro slow-release physicochemical properties.

中文翻译：

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含有紫杉醇的菊粉硬脂酸酯自组装微棒：HeLa 细胞系中的合成和体外细胞毒性 MTT 测定

介绍

宫颈癌是女性最常见的癌症之一，其死亡率正在迅速上升。紫杉醇等药物用于治疗这种癌症。不幸的是，这种药物的疏水性增加了它的副作用。聚合物微棒是合适的载体，可用于运输疏水性药物，如紫杉醇，并以缓慢和受控的方式释放药物。本研究的目的是将紫杉醇加载到聚合菊粉硬脂酸酯微棒上，并评估这些棒的理化特性、药物释放和细胞毒性。

材料和方法

菊粉与硬脂酰氯在 4-二甲氨基吡啶的存在下反应，直到制成菊粉硬脂酸酯并在纯化后冻干。使用透析方法，将紫杉醇加载到聚合物微棒上，最终配方为 10% 和 20%。研究了制备的棒的表面电荷、形态、加载效率、药物释放以及细胞毒性对 HeLa 细胞系的影响。

结果

在水溶剂中，通过透析法，菊粉硬脂酸酯与紫杉醇相互作用并通过自组装方法产生微棒。SEM 图像证明了微棒的结构。10% 和 20% 棒的表面电荷分别为 - 8.19 和 - 10.5 mV。10%的载药量百分比为6.33%，20%为14.89%。最后，体外药物释放的评价显示药物的持续和缓慢释放。对两种剂型的药物释放图表分析表明，20% 的剂型比 10% 的剂型更适合缓释药物研究。20% 制剂的细胞毒性结果还表明，载药菊糖硬脂酸酯棒在 HeLa 细胞系上的IC ₅₀值为 3.1 μM。

结论

在这项研究中，含有紫杉醇 (20%) 的菊粉硬脂酸酯棒表现出良好的体外缓释理化特性。