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首页> 外文期刊>International Journal of Pharmaceutics >Rational design of polysorbate 80 stabilized human serum albumin nanoparticles tailored for high drug loading and entrapment of irinotecan
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Rational design of polysorbate 80 stabilized human serum albumin nanoparticles tailored for high drug loading and entrapment of irinotecan

机译：用于高药物载荷和Irinotecan的高药物载荷量身定制的聚山梨醇酯80稳定的人血清白蛋白纳米粒子的理性设计

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Human serum albumin (HSA) nanoparticles are considered to be versatile carrier of anticancer agents in efficiently delivering the drug to the tumor site without causing any toxicity. The aim of the study was to develop stable HSA nanoparticles (NPs) of drug irinotecan (Iro) having slightly water solubility and moderate HSA binding. A novel strategy of employing a hydrophilic non-ionic surfactant polysorbate 80 which forms protein-polysorbate 80 complex with increased affinity and improvement in Iro-HSA binding has been used to maximize the loading and entrapment efficiency of Iro in HSA-NPs. Bespoke nanoparticles with entrapment efficiency (79.09%) and drug loading of 9.62% could be achieved with spherical shape and particle size of 77.38 nm, 0.290 polydispersity index and -23.7 mv Zeta potential. The drug entrapment in nanoparticles was confirmed by Differential Scanning Calorimeter, Fourier Transformation Infrared Spectroscopy and Fluorescence Spectroscopy. In vitro release of Iro from NPs showed biphasic-release with initial burst followed by prolonged release upto 24 h. The short-term stability investigation of nanodispersion showed no significant changes in physicochemical properties of NPs. Long-term studies on freeze dried Iro-HSA-NPs indicated good stability of NPs up to 12 months. This is the first report for efficient fabrication of Iro delivery system based on HSA nanoparticles.
机译：人血清白蛋白（HSA）的纳米粒子被认为是通用的抗癌剂的载体在药物有效地输送到肿瘤位点，而不会引起任何毒性。该研究的目的是开发药物依立替康（伊洛）的略微具有水溶性稳定HSA纳米颗粒（NP）和中度HSA结合。使用的亲水性非离子表面活性剂聚山梨醇酯80，其形成的蛋白质 - 聚山梨醇酯80复合物与在伊洛-HSA的亲和力增加和改进的新策略的结合已被用于最大化在HSA纳米粒装载和伊洛的包封率。定制与包封率（79.09％）和9.62％的载药量的纳米颗粒可以与球形形状和77.38纳米粒径，0.290的多分散指数和-23.7 MV Zeta电位来实现。在纳米颗粒中的药物包封通过差示扫描量热，傅里叶变换红外光谱和荧光光谱证实。在从纳米粒子伊洛的体外释放表明双相释放与初始突释，随后延长释放高达24小时。纳米分散体的短期稳定性调查显示，NP的理化性质没有显著的变化。在冻结长期研究伊洛干-HSA纳米粒表明纳米粒子具有良好的稳定性长达12个月。这是基于纳米颗粒HSA伊洛输送系统的有效的制造的第一份报告。

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