Concellón Alberto, San Anselmo María, Hernández-Ainsa Silvia, Romero Pilar, Marcos Mercedes, Serrano José Luis
Departamento de Química Orgánica, Instituto de Nanociencia y Materiales de Aragón (INMA), Universidad de Zaragoza-CSIC, 50009 Zaragoza, Spain.
Department of Chemistry, Massachusetts Institute of Technology, Cambridge, MA 02139, USA.
Polymers (Basel). 2020 Nov 30;12(12):2872. doi: 10.3390/polym12122872.
The design of efficient drug-delivery vehicles remains a big challenge in materials science. Herein, we describe a novel class of amphiphilic hybrid dendrimers that consist of a poly(amidoamine) (PAMAM) dendritic core functionalized with MPA dendrons bearing cholesterol and coumarin moieties. Their self-assembly behavior both in bulk and in water was investigated. All dendrimers exhibited smectic A or hexagonal columnar liquid crystal organizations, depending on the generation of the dendrimer. In water, these dendrimers self-assembled to form stable spherical micelles that could encapsulate Nile Red, a hydrophobic model compound. The cell viability in vitro of the micelles was studied in HeLa cell line, and proved to be non-toxic up to 72 h of incubation. Therefore, these spherical micelles allow the encapsulation of hydrophobic molecules, and at the same time provided fluorescent traceability due to the presence of coumarin units in their chemical structure, demonstrating the potential of these dendrimers as nanocarriers for drug-delivery applications.
高效药物递送载体的设计仍然是材料科学中的一个重大挑战。在此，我们描述了一类新型的两亲性杂化树枝状大分子，其由带有胆固醇和香豆素部分的MPA树枝状分子官能化的聚（酰胺胺）（PAMAM）树枝状核心组成。研究了它们在本体和水中的自组装行为。所有树枝状大分子都表现出近晶A或六方柱状液晶结构，这取决于树枝状大分子的代数。在水中，这些树枝状大分子自组装形成稳定的球形胶束，能够包封疏水性模型化合物尼罗红。在HeLa细胞系中研究了胶束的体外细胞活力，结果证明在长达72小时的孵育时间内是无毒的。因此，这些球形胶束能够包封疏水性分子，同时由于其化学结构中存在香豆素单元而提供荧光可追溯性，证明了这些树枝状大分子作为药物递送应用纳米载体的潜力。
