Chlorambucil Encapsulation into PLGA Nanoparticles and Cytotoxic Effects in Breast Cancer Cell

Diego Juscelino Santos Dias, G. Joanitti, R. Azevedo, Luciano P. Silva, C. Lunardi, A. Gomes
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引用次数: 16

Abstract

The present work aimed to develop and evaluate a colloidal system composed of poly (DL-lactide-co-glycolide) (PLGA) nanoparticles (NPs) associated with chlorambucil (CHB) and its effects on cancer cells. The nanoparticles showed %EE (>92%), a mean particle size in the range of 240 to 334 nm and zeta potential of -16.7 to -26.0 mV. In vitro release profile showed a biphasic pattern, with an initial burst for all formulations. The scanning electron microscopy of CHB-nanoparticles showed regular spherical shapes, smooth surface without aggregations. Differential scanning calorimetry thermograms, UV-vis absorption, fluorescence emission and Fourier transform infrared spectroscopy were performed showing the entrapment of the antitumoral in drug delivery system. CHB encapsulated in PLGA nanoparticles decrease the survival rates of the breast cancer cells: 68.9% reduction of cell viability on MCF-7 cell line and 59.7% on NIH3T3. Our results indicated that polymeric nanoparticles produced by classical methods are efficient drug delivery systems for CHB.
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氯吡肟包埋于聚乳酸纳米颗粒及对乳腺癌细胞的细胞毒性作用
本研究旨在建立和评价由聚乳酸-羟基乙酸酯(PLGA)纳米颗粒(NPs)与氯苯(CHB)联合组成的胶体体系及其对癌细胞的影响。纳米颗粒的EE为%(>92%),平均粒径为240 ~ 334 nm, zeta电位为-16.7 ~ -26.0 mV。体外释放谱呈双相模式,所有制剂均有初始爆发。纳米chb纳米颗粒的扫描电镜显示为规则的球形,表面光滑,无聚集。差示扫描量热图、紫外-可见吸收、荧光发射和傅里叶变换红外光谱显示了抗肿瘤药物在给药系统中的包裹性。PLGA纳米颗粒包埋的CHB可降低乳腺癌细胞的存活率:MCF-7细胞存活率降低68.9%,NIH3T3细胞存活率降低59.7%。结果表明,采用传统方法制备的高分子纳米颗粒是一种有效的慢性乙型肝炎药物递送系统。
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