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Niclosamide encapsulated polymeric nanocarriers for targeted cancer therapy

机译:Niclosamide封装的聚合物纳米载体用于靶向癌症治疗

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Localized cancer rates are on an upsurge, severely affecting mankind across the globe. Timely diagnosis and adopting appropriate treatment strategies could improve the quality of life significantly reducing the mortality and morbidity rates. Recently, nanotherapeutics has precipitously shown increased efficacy for controlling abnormal tissue growth in certain sites in the body, among which ligand functionalized nanoparticles (NP) have caught much attention for improved survival statistics via active targeting. Our focus was to repurpose the antihelminthic drug, niclosamide (NIC), which could aid in inhibiting the abnormal growth of cells restricted to a specific region. The work here presents a one-pot synthesis of niclosamide encapsulated, hyaluronic acid functionalized core–shell nanocarriers [(NIC-PLGA NP)HA] for active targeting of localized cancer. The synthesized nanocarriers were found to possess spherical morphology with mean size of 150.8 ± 9 nm and zeta potential of ?24.9 ± 7.21 mV. The encapsulation efficiency was found to be 79.19 ± 0.16% with a loading efficiency of 7.19 ± 0.01%. The nanohybrids exhibited extreme cytocompatibility upon testing with MDA-MB-231 and L929 cell lines. The rate of cancer cell elimination was approximately 85% with targeted cell imaging results being highly convincing. [(NIC-PLGA NP)HA] demonstrates increased cellular uptake leading to a hike in reactive oxygen species (ROS) generation, combating tumour cells aiding in the localized treatment of cancer and associated therapy.
机译:局部癌症发病率呈上升趋势,严重影响着全球人类。及时诊断并采取适当的治疗策略可以改善生活质量,从而大大降低死亡率和发病率。近来,纳米治疗剂已显示出增强的控制体内某些部位异常组织生长的功效,其中配体官能化的纳米颗粒(NP)引起了人们的广泛关注,它们通过主动靶向提高了生存率。我们的重点是重新利用抗蠕虫药niclosamide(NIC),该药物可帮助抑制局限于特定区域的细胞异常生长。这里的工作提出了一种一锅合成的烟酰胺包裹的透明质酸功能化核壳纳米载体[(NIC-PLGA NP)HA],用于局部靶向癌症。发现合成的纳米载体具有球形形态,平均尺寸为150.8±9nm,ζ电势为〜24.9±7.21mV。发现封装效率为79.19±0.16%,负载效率为7.19±0.01%。经MDA-MB-231和L929细胞系测试后,纳米杂化物表现出极强的细胞相容性。癌细胞消除率约为85%,靶向细胞成像结果令人信服。 [(NIC-PLGA NP)HA]证明细胞摄取增加,导致活性氧(ROS)产生增加,与肿瘤细胞作斗争,有助于癌症的局部治疗和相关治疗。

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