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载有AP9-cd的固体脂质纳米粒在人白血病Molt-4细胞和实验性肿瘤中的增强抗癌潜力。

The augmented anticancer potential of AP9-cd loaded solid lipid nanoparticles in human leukemia Molt-4 cells and experimental tumor.

作者信息

Bhushan Shashi, Kakkar Vandita, Pal Harish Chandra, Mondhe D M, Kaur Indu Pal

机构信息

Indian Institute of Integrative Medicine, CSIR, Canal Road, Jammu, 180001, India.

University Institute of Pharmaceutical Sciences, Panjab University, Chandigarh, 160014, India.

出版信息

Chem Biol Interact. 2016 Jan 25;244:84-93. doi: 10.1016/j.cbi.2015.11.022. Epub 2015 Nov 24.

Abstract

AP9-cd, a novel lignan composition from Cedrus deodara has significant anticancer potential, and to further enhance its activity, it was lucratively encumbered into solid lipid nanoparticles (SLNs). These nanoparticles were formulated by micro-emulsion technique with 70% drug trap competence. AP9-cd-SLNs were regular, solid, globular particles in the range of 100-200 nm, which were confirmed by electron microscopic studies. Moreover, AP9-cd-SLNs were found to be stable for up to six months in terms of color, particle size, zeta potential, drug content and entrapment. AP9-cd-SLNs have 30-50% higher cytotoxic and apoptotic potential than the AP9-cd alone. The augmented anticancer potential of AP9-cd-SLNs was observed in cytotoxic IC50 value, apoptosis signaling cascade and in Ehrlich ascites tumor (EAT) model. AP9-cd-SLNs induce apoptosis in Molt-4 cells via both intrinsic and extrinsic pathway. Moreover, the dummy nanoparticles (SLNs without AP9-cd) did not have any cytotoxic effect in cancer as well as in normal cells. Consequently, SLNs of AP9-cd significantly augment the apoptotic and antitumor potential of AP9-cd. The present study provides a podium for ornamental the remedial latent via novel delivery systems like solid lipid nanoparticles.

摘要

AP9-cd是一种从喜马拉雅雪松中提取的新型木脂素成分,具有显著的抗癌潜力。为进一步增强其活性,将其成功负载于固体脂质纳米粒(SLNs)中。这些纳米粒采用微乳技术制备,药物包封率达70%。通过电子显微镜研究证实,AP9-cd-SLNs为规则、固态、球形颗粒,粒径范围在100 - 200纳米。此外,AP9-cd-SLNs在颜色、粒径、zeta电位、药物含量和包封率方面长达六个月保持稳定。AP9-cd-SLNs的细胞毒性和凋亡潜力比单独的AP9-cd高30 - 50%。在细胞毒性IC50值、凋亡信号级联反应以及艾氏腹水瘤(EAT)模型中均观察到AP9-cd-SLNs增强的抗癌潜力。AP9-cd-SLNs通过内在和外在途径诱导Molt-4细胞凋亡。此外,空白纳米粒(不含AP9-cd的SLNs)在癌细胞和正常细胞中均无任何细胞毒性作用。因此,AP9-cd的SLNs显著增强了AP9-cd的凋亡和抗肿瘤潜力。本研究为通过固体脂质纳米粒等新型给药系统探索治疗潜力提供了一个平台。

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