Development of Parvifloron D-loaded Smart Nanoparticles to Target Pancreatic Cancer.

PHARMACEUTICS(2018)

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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 mu M, 11.9 +/- 0.7 mu M, 21.6 +/- 0.5, 34.3 +/- 4.1 mu M,35.1 +/- 2.2 mu M and 32.1 +/- 4.3 mu M 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.
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关键词
Plectranthus ecklonii,Parvifloron D,cytotoxicity,pancreatic cancer,nanoparticles
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