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基于葡萄糖醛酸的表面活性剂的类脂囊泡作为癌症治疗的新型载体:制备、表征和生物学性质。

Niosomes from glucuronic acid-based surfactant as new carriers for cancer therapy: preparation, characterization and biological properties.

机构信息

Dipartimento di Farmacia e Scienze della Salute e della Nutrizione, Università della Calabria, Edificio Polifunzionale, Arcavacata di Rende, 87036 Cosenza, Italy; Dipartimento di Ingegneria Informatica, Modellistica, Elettronica e Sistemistica, Università della Calabria, Via P. Bucci Cubo 39/C, Arcavacata di Rende, 87036 Cosenza, Italy.

Dipartimento di Scienze della Salute, Università Magna Graecia, Via T. Campanella 115, 88100 Catanzaro, Italy.

出版信息

Colloids Surf B Biointerfaces. 2014 Jun 1;118:7-13. doi: 10.1016/j.colsurfb.2014.03.016. Epub 2014 Mar 15.

DOI:10.1016/j.colsurfb.2014.03.016
PMID:24709252
Abstract

Niosomes are vesicular systems composed of surfactant molecules, claimed to be used as drug delivery carriers thanks to their physico-chemical and biological properties. The aim of this work was to design niosomes obtained with a surfactant synthesized from glucuronic acid. Doxorubicin and 5FU were used as model drugs. Niosomes were prepared with different ratios between surfactant and cholesterol, and characterized in terms of size, morphology, drugs entrapment efficiency and in vitro releases, to identify the optimal formulation to be used in pharmaceutical fields. In addition, the hemolytic activity of all formulations have been also evaluated. Results showed that dodecylglucuronamide surfactant was able to produce vesicular systems with or without the presence of cholesterol. Niosomes resulted regular in size and shape and they have been found to encapsulate and release in a controlled manner both doxorubicin and 5-fluorouracil. Hemolytic tests showed that the capability of disrupting erythrocyte only depend on the size of colloidal aggregates. Finally, our formulations could be potentially used as antitumoral delivery systems in anticancer therapy.

摘要

尼欧斯omes 是由表面活性剂分子组成的囊泡系统,由于其物理化学和生物学特性,据称可作为药物传递载体使用。本工作的目的是设计由葡糖醛酸合成的表面活性剂获得的尼欧斯omes。阿霉素和 5FU 被用作模型药物。用不同的表面活性剂与胆固醇的比例制备尼欧斯omes,并对其大小、形态、药物包封效率和体外释放进行了表征,以确定可用于制药领域的最佳配方。此外,还评估了所有配方的溶血活性。结果表明,十二烷基葡糖酰胺表面活性剂能够在有或没有胆固醇的情况下产生囊泡系统。尼欧斯omes 大小和形状规则,并且已经发现能够以受控的方式包封和释放阿霉素和 5-氟尿嘧啶。溶血试验表明,破坏红细胞的能力仅取决于胶体聚集体的大小。最后,我们的配方可潜在地用作抗癌治疗中的抗肿瘤递药系统。

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