当前位置: X-MOL 学术Toxicol. Res. › 论文详情
Our official English website, www.x-mol.net, welcomes your feedback! (Note: you will need to create a separate account there.)
Cell to rodent: toxicological profiling of folate grafted thiomer enveloped nanoliposomes
Toxicology Research ( IF 2.2 ) Pub Date : 2017-07-24 00:00:00 , DOI: 10.1039/c7tx00146k
Muhammad Farhan Sohail 1, 2, 3, 4 , Hafiz Shoaib Sarwar 1 , Ibrahim Javed 3 , Akhtar Nadhman 5 , Syed Zajif Hussain 3 , Hamid Saeed 6 , Abida Raza 7 , Nadeem Irfan Bukhari 6 , Irshad Hussain 3 , Gul Shahnaz 1
Affiliation  

Polymeric nanomaterials, hybridized with lipid components, e.g. phosphocholine or fatty acids, are currently being explored for efficient nano-platforms for hydrophobic drugs. However, their toxicology and toxicokinetics need to be established before enabling their clinical potential. The aim of this study was to investigate the toxicological profile of thiomer enveloped hybrid nanoliposomes (ENLs) and bare nanoliposomes (NLs), loaded with docetaxel (DTX) hydrophobic drug, biocompatible nano-carriers for therapeutic cargo. The in vitro toxicity of hybrid ENLs and NLs was evaluated towards the HCT-116 colon cancer cell line. Biocompatibility was explored against macrophages and acute oral toxicity was examined in mice for 14 days. The anticancer IC50 for ENLs was 0.148 μg ml−1 compared with 2.38 μg ml−1 for pure docetaxel (DTX). The human macrophage viability remained above 65% and demonstrated a high level of biocompatibility and safety of ENLs. In vivo acute oral toxicity showed slight changes in serum biochemistry and haematology but no significant toxicities were observed referring to the safety of DTX loaded hybrid ENLs. On histological examination, no lesions were determined on the liver, heart and kidney. These studies showed that hybrid ENLs can serve as a safe and biocompatible platform for oral delivery of hydrophobic drugs.

中文翻译:


细胞到啮齿动物:叶酸接枝硫聚体包封纳米脂质体的毒理学分析



目前正在探索与脂质成分(例如磷酸胆碱或脂肪酸)杂交的聚合物纳米材料,以用于疏水性药物的有效纳米平台。然而,在发挥其临床潜力之前,需要确定它们的毒理学和毒代动力学。本研究的目的是研究硫柳汞包封的混合纳米脂质体(ENL)和裸纳米脂质体(NL)的毒理学特征,负载多西紫杉醇(DTX)疏水性药物,作为治疗货物的生物相容性纳米载体。评估了杂种 ENL 和 NL 对 HCT-116 结肠癌细胞系的体外毒性。探索了针对巨噬细胞的生物相容性,并在小鼠中检查了 14 天的急性口服毒性。 ENL的抗癌IC 50为0.148 μg ml -1 ,而纯多西紫杉醇(DTX)的抗癌IC 50 为2.38 μg ml -1 。人类巨噬细胞活力保持在 65% 以上,并表现出 ENL 的高水平生物相容性和安全性。体内急性口服毒性显示血清生化和血液学发生轻微变化,但就负载 DTX 的混合 ENL 的安全性而言,未观察到显着毒性。组织学检查,肝脏、心脏和肾脏未发现病变。这些研究表明,混合 ENL 可以作为疏水性药物口服给药的安全且生物相容的平台。
更新日期:2017-08-03
down
wechat
bug