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首页> 外文期刊>RSC Advances >Bionanotherapeutics: niclosamide encapsulated albumin nanoparticles as a novel drug delivery system for cancer therapy
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Bionanotherapeutics: niclosamide encapsulated albumin nanoparticles as a novel drug delivery system for cancer therapy

机译：生物纳米疗法：烟酰胺包裹的白蛋白纳米颗粒作为一种新型的癌症治疗药物递送系统

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One of the major unresolved challenges among the scientific community is to develop anticancer drugs that are safe and effective. A large number of anticancer drugs have been screened so far in this campaign. Among them niclosamide has shown tremendous anti-cancer potential as demonstrated in a surfeit of human cancer cell lines and animal models. But the extreme hydrophobicity and consequently, minimal systemic bioavailability associated with this drug limited its widespread clinical applications. Nanoparticles based drug delivery systems have the potential for realizing water soluble formulation of highly hydrophobic anticancer drugs like niclosamide, thus evading the drawbacks of poor solubility. In this work niclosamide was encapsulated into albumin nanoparticles through a desolvation method to improve its scope of application in cancer therapy. Physico-chemical characterization confirms that the prepared nanoparticles are spherical, highly monodispersed, and stable in aqueous systems. These drug encapsulated albumin nanoparticles, unlike the free drug demonstrate better in vitro therapeutic efficacy against human lung and breast cancer cell lines, as assessed by cell viability assay and morphological analyses. Further, the proficient induction of apoptosis by these nanoparticles was confirmed by semiquantitative RT-PCR. This work open up a new avenue to extend the clinical gamut of this effectual agent by enabling its aqueous dispersion.
机译：科学界尚未解决的主要挑战之一是开发安全有效的抗癌药物。迄今为止，在这项运动中已经筛选出了大量的抗癌药物。其中，如大量的人类癌细胞系和动物模型所证明的那样，niclosamide具有巨大的抗癌潜力。但是与该药物相关的极高的疏水性以及因此最小的全身生物利用度限制了其广泛的临床应用。基于纳米颗粒的药物递送系统具有实现高度疏水性抗癌药物如尼克洛沙胺的水溶性制剂的潜力，因此避免了溶解性差的缺点。在这项工作中，尼克洛沙胺通过去溶剂化方法被封装到白蛋白纳米颗粒中，以改善其在癌症治疗中的应用范围。物理化学特征证实，所制备的纳米颗粒为球形，高度单分散且在水性体系中稳定。如通过细胞生存力测定和形态分析所评估的，与游离药物不同，这些药物包封的白蛋白纳米颗粒表现出更好的针对人肺癌和乳腺癌细胞系的体外治疗功效。此外，通过半定量RT-PCR证实了这些纳米颗粒对细胞凋亡的有效诱导。这项工作开辟了一条新途径，可通过使其水分散液来扩展该有效剂的临床范围。

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