Lozano-García Rebeca, Quintana-Sánchez Sara, Benito-Martínez Selma, Torrado Guillermo, Guarnizo-Herrero Víctor, Martínez-Alonso Borja, Pascual Gemma, Pérez-Köhler Bárbara, Sánchez-Nieves Javier, de la Mata F Javier
Universidad de Alcalá (UAH), Departamento de Química Orgánica y Química Inorgánica, Edificio de Farmacia, Research Institute in Chemistry "Andrés M. del Río" (IQAR), Campus Universitario, 28805 Alcalá de Henares, Madrid, Spain.
Networking Research Centre for Bioengineering, Biomaterials and Nanomedicine (CIBER-BBN), Instituto de Salud Carlos III, 28029 Madrid, Spain.
ACS Appl Polym Mater. 2025 Jul 23;7(15):10026-10037. doi: 10.1021/acsapm.5c01718. eCollection 2025 Aug 8.
Skin wounds are an important factor in developing bacterial infection, especially for chronic wounds. In this case, the exposure to long traditional antibacterial-based treatments can lead to the appearance of resistance to these drugs. This situation makes the search for alternatives to attack these infections essential, as it is the use of cationic multivalent systems. Here, we discussed the antibacterial and biological properties of different cationic carbosilane (CBS) dendrimers against () and () as models of Gram-positive and Gram-negative bacteria, respectively. Dendrimers are a type of multivalent molecule with a well-defined structure. The CBS dendrimers used in this work differ in several modifications that affect the hydrophobic/hydrophilic balance, which is very relevant to achieve bactericidal activity. These structural changes are the position of a short alkyl chain, in the internal dendritic structure or on the outer ammonium groups, the presence of a polyethylene glycol (PEG) chain instead of a cationic function, or in the vicinal moieties of the cationic functions, sulfur atoms or sulfone units. The studies allowed the selection of some dendrimers, all of them with the inner long chain and trimethylammonium (-NMe ) groups, as active ingredients of a topical cream (water in oil, W/O). The antibacterial and biological properties of the creams were also tested against bacteria because it is the most common pathogen involved in skin infections. We observed different abilities of the dendrimers to be released from the cream, depending on the dendrimer structure, and as a consequence, different antibacterial properties of the creams. Finally, an analysis of the physicochemical properties of the best formulation was also done.
皮肤伤口是引发细菌感染的重要因素,尤其是对于慢性伤口而言。在这种情况下,长期使用传统的基于抗菌药物的治疗方法可能会导致细菌对这些药物产生耐药性。这种情况使得寻找治疗这些感染的替代方法变得至关重要,阳离子多价体系的应用便是其中之一。在此,我们讨论了不同阳离子碳硅烷(CBS)树枝状大分子分别针对革兰氏阳性菌和革兰氏阴性菌模型()和()的抗菌及生物学特性。树枝状大分子是一类具有明确结构的多价分子。本研究中使用的CBS树枝状大分子在几个方面存在差异,这些差异会影响疏水/亲水平衡,而这对于实现杀菌活性非常关键。这些结构变化包括短烷基链在内部树枝状结构或外部铵基团上的位置、用聚乙二醇(PEG)链取代阳离子官能团、阳离子官能团的邻位部分存在硫原子或砜单元。这些研究使得我们能够选择一些树枝状大分子,它们都具有内部长链和三甲基铵(-NMe )基团,作为一种外用乳膏(油包水,W/O)的活性成分。还针对细菌测试了该乳膏的抗菌及生物学特性,因为它是皮肤感染中最常见的病原体。我们观察到,根据树枝状大分子的结构不同,其从乳膏中释放的能力也不同,相应地,乳膏的抗菌特性也有所不同。最后,还对最佳配方的物理化学性质进行了分析。