Niclosamide loaded cationic Solid Lipid Nanoparticles for treatment of Cancer

N. Jain, R. Srivastava, V. Naidu
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引用次数: 1

Abstract

Niclosamide (NIC), an anthelminthic drug exhibits poor oral bioavailability due to hydrophobic nature which limits its in vivo application. In recent times, NIC has been reported to exhibit anticancer activity against wide range of tumors. Solid Lipid Nanoparticles (SLNs) of NIC were prepared using solid lipid Glyceryl monostearate, charge modifier stearyl amine, soya lecithin, and tween 80 by emulsion solvent evaporation technique. The SLNs were characterized for their size and zeta potential using Zetasizer. Whereas, the morphology was studied using TEM analysis. The results suggested the formation of positively charged SLNs with a size range of 197.3±18.08nm and zeta potential of +10±3.43 mV. The interaction of the excipients with the drug was studied using FTIR which suggested their compatibility with NIC. The entrapment efficiency and loading efficiency was determined and found to be 75.64±8.49% and 8.16±0.31% respectively. The results of the drug release study indicated the prolonged and sustained release of NIC over a period of 24h. Hence, the NIC loaded solid lipid nanoparticles can deliver the drug for sustained period of time which can be used in the treatment of Cancer.
氯硝柳胺负载的阳离子固体脂质纳米颗粒治疗癌症
氯硝柳胺(Niclosamide, NIC)是一种驱虫药物,由于其疏水性,口服生物利用度较差,限制了其在体内的应用。近年来,NIC已被报道对多种肿瘤表现出抗癌活性。以固体脂质单硬脂酸甘油酯、电荷调节剂硬脂酰胺、大豆卵磷脂和间烯80为原料,采用乳液溶剂蒸发法制备了NIC固体脂质纳米颗粒。用Zetasizer对sln的大小和zeta电位进行了表征。利用透射电镜对其形貌进行了研究。结果表明,所制得的sln带正电荷,尺寸范围为197.3±18.08nm, zeta电位为+10±3.43 mV。用FTIR研究了辅料与药物的相互作用,证实了辅料与NIC的配伍性。捕集效率为75.64±8.49%,载虫效率为8.16±0.31%。释放研究结果表明,NIC的释放时间延长,持续时间为24h。因此,NIC负载的固体脂质纳米颗粒可以持续递送药物一段时间,可用于治疗癌症。
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