Fabrication, characterization and bioevaluation of silibinin loaded chitosan nanoparticles
Fabrication, characterization and bioevaluation of silibinin loaded chitosan nanoparticles
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DOI：
10.1016/j.ijbiomac.2014.05.035
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发表时间：
2014-08-01
影响因子：
8.2
通讯作者：
Tiwari, Ashok K.
中科院分区：
文献类型：
--
作者：
Pooja, Deep;Bikkina, Dileep J. Babu;Tiwari, Ashok K.
水飞蓟宾具有多种生物活性。然而，其疏水性质限制了其生物利用度，从而损害了体内生物活性。基于纳米颗粒的这些分子的递送已经成为解决这些问题的新技术。壳聚糖的生物可降解性、相容性和粘附性吸引了其作为生物活性分子载体的适用性。本研究以壳聚糖-三聚磷酸钠为载体制备水飞蓟宾微胶囊。研究了水飞蓟宾包封壳聚糖-三聚磷酸钠纳米颗粒的粒径、形貌、zeta电位和包封率。还评价了制剂的体外细胞毒性活性。优化后的水飞蓟宾壳聚糖纳米粒粒径为263.7 ± 4.1 nm，zeta电位为37.4 ± 1.57 mV。纳米颗粒显示出高的水飞蓟宾包封率（82.94 +/-1.82%）。FTIR分析表明水飞蓟宾与壳聚糖之间没有发生化学作用。粉末X-射线衍射分析揭示了胶囊化后水飞蓟宾的物理状态发生了变化。利用TEM和DSC分析确定表面形态和热行为。与单独的水飞蓟宾相比，包封的水飞蓟宾显示出增加的溶解和对人前列腺癌细胞（DU 145）更好的细胞毒性。(C)2014爱思唯尔有限公司版权所有。
Silibinin is reported to possess multiple biological activities. However, its hydrophobic nature limits its bioavailability compromising in vivo biological activities. Nanoparticles-based delivery of such molecules has emerged as new technique to resolve these issues. Bio-degradable, compatible and adhesive nature of chitosan has recently attracted its suitability as a carrier for biologically active molecules. This study presents fabrication and characterization of chitosan-tripolyphosphate based encapsulation of silibinin. Various preparations of silibinin encapsulated chitosan-tripolyphosphate nanoparticles were studied for particle size, morphology, zeta-potential, and encapsulation efficiencies. Preparations were also evaluated for cytotoxic activities in vitro. The optimized silibinin loaded chitosan nanoparticles were of 263.7 +/- 4.1 nm in particle size with zeta potential 37.4 +/- 1.57 mV. Nanoparticles showed high silibinin encapsulation efficiencies (82.94 +/- 1.82%). No chemical interactions between silibinin and chitosan were observed in FTIR analysis. Powder X-ray diffraction analysis revealed transformed physical state of silibinin after encapsulation. Surface morphology and thermal behaviour were determined using TEM and DSC analysis. Encapsulated silibinin displayed increased dissolution and better cytotoxicity against human prostate cancer cells (DU145) than silibinin alone. (C) 2014 Elsevier B.V. All rights reserved.