Jalilian Milad, Derakhshandeh Katayoun, Kurd Masoumeh, Lashani Hussein
Department of Pharmaceutics, School of Pharmacy, Hamadan University of Medical Sciences, Hamadan, Iran.
Medicinal Plants and Natural Products Research Center, Hamadan University of Medical Sciences, Hamadan, Iran.
Iran J Pharm Res. 2021 Winter;20(1):327-338. doi: 10.22037/ijpr.2020.113436.14302.
The purpose of the current study was to prepare and characterize the targeted solid lipid nanoparticles (SLNs) containing docetaxel (DTX) for prostate cancer treatment. The goal has been achieved by locating anisamide (Anis) ligand on the surface of SLNs, which can interact with the overexpressed sigma receptor on the prostate cancer cells. DTX loaded SLNs were prepared by high shear homogenization and ultra-sonication method and optimized by applying experimental design. The average particle size and the entrapment efficiency of the optimum DTX-SLN were 174 ± 9.1 nm and 83 ± 3.34%, respectively. The results of differential scanning calorimetry showed that DTX had been dispersed as amorphous in the nanocarriers. Scanning electron microscopy (SEM) images confirmed the nanoscale size and spherical shape of the nanoparticles. The cytotoxicity studies have demonstrated that IC of free drug, DTX-SLN and DTX-SLN-Anis was 0.25 ± 0.01, 0.23 ± 0.02, 0.12 ± 0.01 nM on PC3 cell line and 20.9 ± 3.89, 18.74 ± 7.43, and 14.68 ± 5.70 nM on HEK293 cell line, respectively. Targeted DTX-SLN-Anis was acted more effectively on prostate cancer cells in comparison to DTX-SLN and free drug. The results of this study have depicted that the anti-cancer drug loaded in targeted SLNs can be a promising way for cancer treatment. In addition, performing studies will be complementary to these findings.
本研究的目的是制备并表征用于前列腺癌治疗的载多西他赛(DTX)的靶向固体脂质纳米粒(SLNs)。通过在SLNs表面定位茴香酰胺(Anis)配体实现了这一目标,该配体可与前列腺癌细胞上过表达的σ受体相互作用。采用高剪切均质化和超声处理方法制备了载DTX的SLNs,并通过实验设计进行了优化。最佳DTX-SLN的平均粒径和包封率分别为174±9.1nm和83±3.34%。差示扫描量热法结果表明,DTX在纳米载体中以无定形形式分散。扫描电子显微镜(SEM)图像证实了纳米颗粒的纳米级尺寸和球形形状。细胞毒性研究表明,游离药物、DTX-SLN和DTX-SLN-Anis对PC3细胞系的IC50分别为0.25±0.01、0.23±0.02、0.12±0.01nM,对HEK293细胞系的IC50分别为20.9±3.89、18.74±7.43和14.68±5.70nM。与DTX-SLN和游离药物相比,靶向DTX-SLN-Anis对前列腺癌细胞的作用更有效。本研究结果表明,载于靶向SLNs中的抗癌药物可能是一种有前景的癌症治疗方法。此外,开展进一步研究将补充这些发现。