当前位置: X-MOL 学术Pharmaceutics › 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.)
Design and Characterization of Glyceryl Monooleate-Nanostructures Containing Doxorubicin Hydrochloride
Pharmaceutics ( IF 5.4 ) Pub Date : 2020-10-24 , DOI: 10.3390/pharmaceutics12111017
Agnese Gagliardi , Donato Cosco , Betty P. Udongo , Luciana Dini , Giuseppe Viglietto , Donatella Paolino

Glyceryl monooleate (GMO) is one of the most popular amphiphilic lipids, which, in the presence of different amounts of water and a proper amount of stabilizer, can promote the development of well defined, thermodynamically stable nanostructures, called lyotropic liquid crystal dispersions. The aim of this study is based on the design, characterization, and evaluation of the cytotoxicity of lyotropic liquid crystal nanostructures containing a model anticancer drug such as doxorubicin hydrochloride. The drug is efficiently retained by the GMO nanosystems by a remote loading approach. The nanostructures prepared with different non-ionic surfactants (poloxamers and polysorbates) are characterized by different physico-chemical features as a function of several parameters, i.e., serum stability, temperature, and different pH values, as well as the amount of cryoprotectants used to obtain suitable freeze-dried systems. The nanostructures prepared with poloxamer 407 used as a stabilizer show an increased toxicity of the entrapped drug on breast cancer cell lines (MCF-7 and MDA-MB-231) due to their ability to sensitize multidrug-resistant (MDR) tumor cells through the inhibition of specific drug efflux transporters. Moreover, the interaction between the nanostructures and the cells occurs after just a few hours, evidencing a huge cellular uptake of the nanosystems.

中文翻译:

盐酸阿霉素甘油单油酸酯纳米结构的设计与表征

甘油单油酸酯(GMO)是最流行的两亲脂质之一,在存在不同量的水和适量的稳定剂的情况下,它们可以促进定义明确的,热力学稳定的纳米结构的发展,称为溶致液晶分散体。这项研究的目的是基于对含有模型抗癌药(例如盐酸阿霉素)的溶致液晶纳米结构的细胞毒性的设计,表征和评估。该药物可通过远程装载方法被GMO纳米系统有效保留。用不同的非离子型表面活性剂(泊洛沙姆和聚山梨酯)制备的纳米结构的特征在于,根据几个参数(例如血清稳定性,温度和不同的pH值)的不同,其理化特性也不同,以及用于获得合适的冻干系统的冷冻保护剂的量。用泊洛沙姆407用作稳定剂制备的纳米结构显示出,所包埋的药物对乳腺癌细胞系(MCF-7和MDA-MB-231)的毒性增加,这是因为它们能够通过抗药性增强对多药耐药(MDR)的肿瘤细胞的敏感性。抑制特定药物外排转运蛋白。此外,纳米结构和细胞之间的相互作用仅在几个小时后发生,表明纳米系统被大量细胞吸收。用泊洛沙姆407用作稳定剂制备的纳米结构显示出,所包埋的药物对乳腺癌细胞系(MCF-7和MDA-MB-231)的毒性增加,这是因为它们能够通过抗药性增强对多药耐药(MDR)的肿瘤细胞的敏感性。抑制特定药物外排转运蛋白。此外,纳米结构和细胞之间的相互作用仅在几个小时后发生,表明纳米系统被大量细胞吸收。用泊洛沙姆407用作稳定剂制备的纳米结构显示出,所包埋的药物对乳腺癌细胞系(MCF-7和MDA-MB-231)的毒性增加,这是因为它们能够通过抗药性增强对多药耐药(MDR)的肿瘤细胞的敏感性。抑制特定药物外排转运蛋白。此外,纳米结构和细胞之间的相互作用仅在几个小时后发生,表明纳米系统被大量细胞吸收。
更新日期:2020-10-28
down
wechat
bug