Effects of particle size and surface charge on cellular uptake and biodistribution of polymeric nanoparticles
Effects of particle size and surface charge on cellular uptake and biodistribution of polymeric nanoparticles
复制标题
粒径和表面电荷对聚合物纳米粒子的细胞摄取和生物分布的影响
DOI：
10.1016/j.biomaterials.2010.01.065
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发表时间：
2010-05-01
期刊：
影响因子：
14
通讯作者：
Yin, Chunhua
中科院分区：
文献类型：
--
作者：
He, Chunbai;Hu, Yiping;Yin, Chunhua
为了阐明粒径和表面电荷对聚合物纳米颗粒（NPs）细胞摄取和生物分布的影响，分别以罗丹明B （RhB）标记的羧甲基壳聚糖接枝NPs （RhB- cmcnp）和盐酸壳聚糖接枝NPs （RhB- chnp）作为带负电和带正电的聚合物NPs模型。这些NPs具有明确的粒径（150-500 nm）和Zeta电位（-40 mV - +35 mV）。制备了高包封率的FITC标记的载RhB-CMCNP硫酸鱼精蛋白（FITC- ps）和载RhB-CHNP喜树碱（CPT）。对其在血浆中及对I的荧光稳定性进行了研究，结果表明其足以进行定性和定量分析。表面电荷高、粒径大的NPs被小鼠巨噬细胞吞噬效率高。微小的颗粒大小和表面电荷差异以及不同细胞系对NPs的细胞摄取有显著影响，摄取过程涉及多种机制。体内生物分布表明，微负电荷、粒径为150 nm的NPs更容易在肿瘤中积累。这些结果可为合理设计具有最大治疗效果和可预测体内性能的药物纳米载体提供指导，其中颗粒大小和表面电荷的控制具有重要意义。(C) 2010 Elsevier Ltd.版权所有。
To elucidate the effects of particle size and surface charge on cellular uptake and biodistribution of polymeric nanoparticles (NPs), rhodamine B (RhB) labeled carboxymethyl chitosan grafted NPs (RhB-CMCNP) and chitosan hydrochloride grafted NPs (RhB-CHNP) were developed as the model negatively and positively charged polymeric NPs, respectively. These NPs owned well defined particle sizes (150-500 nm) and Zeta potentials (-40 mV - +35 mV). FITC labeled protamine sulfate (FITC-PS) loaded RhB-CMCNP and camptothecin (CPT) loaded RhB-CHNP with high encapsulation efficiency were prepared. The fluorescence stability in plasma and towards I was investigated, and the result indicated it was sufficient for qualitative and quantitative analysis. NPs with high surface charge and large particle size were phagocytized more efficiently by murine macrophage. Slight particle size and surface charge differences and different cell lines had significant implications in the cellular uptake of NPs, and various mechanisms were involved in the uptake process. In vivo biodistribution suggested that NPs with slight negative charges and particle size of 150 nm were tended to accumulate in tumor more efficiently. These results could serve as a guideline in the rational design of drug nanocarriers with maximized therapeutic efficacy and predictable in vivo properties, in which the control of particle size and surface charge was of significance. (C) 2010 Elsevier Ltd. All rights reserved.