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用于肝癌治疗的混合脂质纳米制剂:载有索拉非尼的纳米脂质体——一项初步研究

Hybrid Lipid Nanoformulations for Hepatoma Therapy: Sorafenib Loaded Nanoliposomes-A Preliminary Study.

作者信息

Bartos Adrian, Iancu Ioana, Ciobanu Lidia, Onaciu Anca, Moldovan Cristian, Moldovan Alin, Moldovan Radu Cristian, Tigu Adrian Bogdan, Stiufiuc Gabriela Fabiola, Toma Valentin, Iancu Cornel, Al Hajjar Nadim, Stiufiuc Rares Ionut

机构信息

Department of Surgery, Regional Institute of Gastroenterology and Hepatology, 400162 Cluj-Napoca, Romania.

Department of Surgery, "Iuliu Hatieganu" University of Medicine and Pharmacy, 400337 Cluj-Napoca, Romania.

出版信息

Nanomaterials (Basel). 2022 Aug 17;12(16):2833. doi: 10.3390/nano12162833.

Abstract

Sorafenib is a multikinase inhibitor that has received increasing attention due to its high efficacy in hepatocellular carcinoma treatment. However, its poor pharmacokinetic properties (limited water solubility, rapid elimination, and metabolism) still represent major bottlenecks that need to be overcome in order to improve Sorafenib's clinical application. In this paper, we propose a nanotechnology-based hybrid formulation that has the potential to overcome these challenges: sorafenib-loaded nanoliposomes. Sorafenib molecules have been incorporated into the hydrophobic lipidic bilayer during the synthesis process of nanoliposomes using an original procedure developed in our laboratory and, to the best of our knowledge, this is the first paper reporting this type of analysis. The liposomal hybrid formulations have been characterized by transmission electron microscopy (TEM), dynamic light scattering (DLS), and nanoparticle tracking analysis (NTA) that provided useful information concerning their shape, size, zeta-potential, and concentration. The therapeutic efficacy of the nanohybrids has been evaluated on a normal cell line (LX2) and two hepatocarcinoma cell lines, SK-HEP-1 and HepG2, respectively.

摘要

索拉非尼是一种多激酶抑制剂,因其在肝细胞癌治疗中的高效性而受到越来越多的关注。然而,其较差的药代动力学性质(有限的水溶性、快速消除和代谢)仍然是主要瓶颈,为了改善索拉非尼的临床应用,这些瓶颈需要被克服。在本文中,我们提出了一种基于纳米技术的混合制剂,它有可能克服这些挑战:载索拉非尼纳米脂质体。在纳米脂质体的合成过程中,通过我们实验室开发的原始方法,索拉非尼分子已被纳入疏水脂质双层,据我们所知,这是第一篇报道此类分析的论文。脂质体混合制剂已通过透射电子显微镜(TEM)、动态光散射(DLS)和纳米颗粒跟踪分析(NTA)进行了表征,这些分析提供了有关其形状、大小、zeta电位和浓度的有用信息。分别在正常细胞系(LX2)和两种肝癌细胞系SK-HEP-1和HepG2上评估了纳米杂交体的治疗效果。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/b97c/9414144/9bc650174e50/nanomaterials-12-02833-g001.jpg

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