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Development of Parvifloron D-Loaded Smart Nanoparticles to Target Pancreatic Cancer

机译:Parvifloron D加载智能纳米颗粒靶向胰腺癌的发展。

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摘要

Pancreatic cancer is the eighth leading cause of cancer death worldwide. For this reason, the development of more effective therapies is a major concern for the scientific community. Accordingly, plants belonging to Plectranthus genus and their isolated compounds, such as Parvifloron D, were found to have cytotoxic and antiproliferative activities. However, Parvifloron D is a very low water-soluble compound. Thus, nanotechnology can be a promising delivery system to enhance drug solubility and targeted delivery. The extraction of Parvifloron D from P. ecklonii was optimized through an acetone ultrasound-assisted method and isolated by Flash-Dry Column Chromatography. Then, its antiproliferative effect was selectivity evaluated against different cell lines (IC50 of 0.15 ± 0.05 μM, 11.9 ± 0.7 μM, 21.6 ± 0.5, 34.3 ± 4.1 μM, 35.1 ± 2.2 μM and 32.1 ± 4.3 μM for BxPC3, PANC-1, Ins1-E, MCF-7, HaCat and Caco-2, respectively). To obtain an optimized stable Parvifloron D pharmaceutical dosage form, albumin nanoparticles were produced through a desolvation method (yield of encapsulation of 91.2%) and characterized in terms of size (165 nm; PI 0.11), zeta potential (−7.88 mV) and morphology. In conclusion, Parvifloron D can be efficiently obtained from P. ecklonii and it has shown selective cytotoxicity to pancreatic cell lines. Parvifloron D nanoencapsulation can be considered as a possible efficient alternative approach in the treatment of pancreatic cancer.
机译:胰腺癌是全球癌症死亡的第八大主要原因。因此,开发更有效的疗法是科学界的主要关注。因此,发现属于凤尾草属的植物及其分离的化合物如Parvifloron D具有细胞毒性和抗增殖活性。但是,Parvifloron D是水溶性很低的化合物。因此,纳米技术可以成为增强药物溶解度和靶向递送的有前途的递送系统。通过丙酮超声辅助法对P. ecklonii中Parvifloron D的提取进行了优化,并通过快速干柱色谱法进行了分离。然后,针对不同细胞系评估其抗增殖作用的选择性(IC50为0.15±0.05μM,11.9±0.7μM,21.6±0.5、34.3±4.1μM,35.1±2.2μM和32.1±4.3μM,对于BxPC3,PANC-1, Ins1-E,MCF-7,HaCat和Caco-2)。为了获得优化的稳定的Parvifloron D药物剂型,通过去溶剂化方法(包封率为91.2%)制备了白蛋白纳米颗粒,并通过尺寸(165 nm; PI 0.11),ζ电位(-7.88 mV)和形态表征。综上所述,Parvifloron D可以从P. ecklonii有效地获得,并且已经显示出对胰腺细胞系的选择性细胞毒性。 Parvifloron D纳米囊化可以被认为是治疗胰腺癌的一种可能有效的替代方法。

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