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用于递送非瑟酮的白蛋白基纳米颗粒的制备及其细胞毒性活性评估。

Preparation of albumin based nanoparticles for delivery of fisetin and evaluation of its cytotoxic activity.

作者信息

Ghosh Pooja, Singha Roy Atanu, Chaudhury Susmitnarayan, Jana Saikat Kumar, Chaudhury Koel, Dasgupta Swagata

机构信息

Department of Chemistry, Indian Institute of Technology Kharagpur, Kharagpur 721302, India.

School of Medical Science and Technology, Indian Institute of Technology Kharagpur, Kharagpur 721302, India.

出版信息

Int J Biol Macromol. 2016 May;86:408-17. doi: 10.1016/j.ijbiomac.2016.01.082. Epub 2016 Jan 25.

Abstract

Fisetin is a well known flavonoid that shows several properties such as antioxidant, antiviral and anticancer activities. Its use in the pharmaceutical field is limited due to its poor aqueous solubility which results in poor bioavailability and poor permeability. The aim of our present study is to prepare fisetin loaded human serum albumin nanoparticles to improve its bioavailability. The nanoparticles were prepared by a desolvation method and characterized by spectroscopic and microscopic techniques. The particles were smooth and spherical in nature with an average size of 220 ± 8 nm. The encapsulation efficiency was found to be 84%. The in vitro release profile showed a biphasic pattern and the release rate increases with increase in ionic strength of solution. We have also confirmed the antioxidant activity of the prepared nanoparticles by a DPPH (2,2-diphenyl-1-picrylhydrazyl) assay. Further its anticancer activity was evaluated using MCF-7 breast cancer cell lines. Our findings suggest that fisetin loaded HSA nanoparticles could be used to transfer fisetin to target areas under specific conditions and thus may find use as a delivery vehicle for the flavonoid.

摘要

漆黄素是一种著名的黄酮类化合物,具有抗氧化、抗病毒和抗癌等多种特性。由于其水溶性差,导致生物利用度低和渗透性差,其在制药领域的应用受到限制。我们目前研究的目的是制备负载漆黄素的人血清白蛋白纳米颗粒,以提高其生物利用度。纳米颗粒通过去溶剂化方法制备,并通过光谱和显微镜技术进行表征。颗粒本质上是光滑的球形,平均尺寸为220±8纳米。包封率为84%。体外释放曲线呈现双相模式,释放速率随溶液离子强度的增加而增加。我们还通过DPPH(2,2-二苯基-1-苦基肼)测定法证实了所制备纳米颗粒的抗氧化活性。此外,使用MCF-7乳腺癌细胞系评估了其抗癌活性。我们的研究结果表明,负载漆黄素的人血清白蛋白纳米颗粒可用于在特定条件下将漆黄素转运至靶区域,因此可能用作该黄酮类化合物的递送载体。

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