Broad spectrum therapeutic potential of curcumin is usually hampered by its photodegradation and low bioavailability. Present investigation was designed with an objective to develop transferrin-mediated solid lipid nanoparticles (Tf-C-SLN) resistant to the photostability and capable of enhancing the bioavailability by targeted drug delivery to elicit anticancer activity against SH-SY5Y neuroblastoma cells in vitro. Hot homogenization method was used for the formulation of Tf-C-SLN and evaluated physicochemically using parameters such as, size, zeta potential, entrapment efficiency and photostability, transmission electron microscopy (TEM), nuclear magnetic resonance (NMR), differential scanning colorimetry (DSC), and in vitro release study. In vitro cytotoxicity and apoptosis investigations were performed using microplate analysis and flow cytometry techniques. The physicochemical characterization confirmed the suitability of formulation method and various parameters therein. TEM investigation revealed the spherical morphology while NMR and DSC study confirmed the entrapment of curcumin inside the nanoparticles. The cytotoxicity, reactive oxygen species, and cell uptake were found to be increased considerably with Tf-C-SLN compared with curcumin-solubilized surfactant solution, and curcumin-loaded SLN (C-SLN) suggesting the targeting effect. AnnexinV-FITC/PI double staining, DNA analysis, caspase detection, and reduced mitochondrial potential confirmed the induction of apoptosis with nanoparticle treatment. Enhanced anticancer activity with Tf-C-SLN compared with curcumin-solubilized surfactant solution and C-SLN was observed from flow cytometry investigations with apoptosis being the major underlying mechanism. The in vitro observations of our investigation are very compelling and concrete to advocate the potential of Tf-C-SLN in enhancing the anticancer effect of curcumin against neuroblastoma in vivo and possible clinical applications.

中文翻译：

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姜黄素与转铁蛋白结合的固体脂质纳米粒的凋亡诱导抗癌作用。

姜黄素的光降解和低生物利用度通常会阻碍其广泛的治疗潜力。设计本研究的目的是开发转铁蛋白介导的固体脂质纳米颗粒（Tf-C-SLN），其对光稳定性具有抵抗力，并能够通过靶向药物递送增强生物利用度，从而在体外引起针对SH-SY5Y神经母细胞瘤细胞的抗癌活性。使用热均质法制备Tf-C-SLN，并使用尺寸，ζ电势，包封率和光稳定性，透射电子显微镜（TEM），核磁共振（NMR），差示扫描比色法（ DSC）和体外释放研究。使用微孔板分析和流式细胞仪技术进行了体外细胞毒性和凋亡研究。物化特性证实了该配制方法和其中各种参数的适用性。TEM研究揭示了球形形态，而NMR和DSC研究证实了姜黄素截留在纳米颗粒内部。与姜黄素增溶的表面活性剂溶液相比，Tf-C-SLN的细胞毒性，活性氧种类和细胞摄取均显着增加，而姜黄素负载的SLN（C-SLN）表明具有靶向作用。AnnexinV-FITC / PI双重染色，DNA分析，半胱天冬酶检测和线粒体电位降低证实了纳米颗粒治疗诱导了细胞凋亡。从流式细胞术研究中观察到，与姜黄素增溶的表面活性剂溶液和C-SLN相比，Tf-C-SLN具有增强的抗癌活性，而凋亡是其主要的潜在机制。我们研究的体外观察非常有说服力，并且可以具体证明Tf-C-SLN在增强姜黄素在体内对神经母细胞瘤的抗癌作用方面的潜力以及可能的临床应用。