Paolino Marco, Licciardi Mariano, Savoca Cristina, Giammona Gaetano, Modica De Mohac Laura, Reale Annalisa, Giuliani Germano, Komber Hartmut, Donati Alessandro, Leone Gemma, Magnani Agnese, Anzini Maurizio, Cappelli Andrea
Dipartimento di Biotecnologie, Chimica e Farmacia (Dipartimento di Eccellenza 2018-2022), Università degli Studi di Siena, Via A. Moro 2, 53100 Siena, Italy.
Dipartimento di Scienze e Tecnologie Biologiche, Chimiche e Farmaceutiche (STEBICEF), Università degli Studi di Palermo, Via Archirafi 32, 90123 Palermo, Italy.
Pharmaceutics. 2019 Dec 12;11(12):675. doi: 10.3390/pharmaceutics11120675.
In order to evaluate the potential of a technology platform based on hyaluronan copolymers grafted with propargylated ferulate fluorophores (HA-FA-Pg) in the development of drug delivery systems, the propargyl groups of HA-FA-Pg derivatives were employed with oleic acid (OA) or stearic acid (SA) residues across a biocompatible hexa(ethylene glycol) (HEG) spacer. The designed materials (i.e., or ) showed clear-cut aggregation features in an aqueous environment, as confirmed by dynamic light scattering (DLS) and transmission electron microscopy (TEM), generating nanoaggregate systems. In fact, and derivatives showed the property to create self-assembled cytocompatible nanostructured aggregates in water, thanks to the simultaneous presence of hydrophilic portions in the polymeric backbone, such as hyaluronic acid, and hydrophobic portions in the side chains. Furthermore, the designed materials interact with living cells showing a high degree of cytocompatibility. The potential ability of nanosystems to load pharmacologically active molecules was assessed by the physical entrapment of olanzapine into both polymeric systems. The drug loading evaluation demonstrated that the nanoparticles are able to incorporate a good quantity of olanzapine, as well as improve drug solubility, release profile, and cytocompatibility.
为了评估基于接枝有炔丙基阿魏酸荧光团的透明质酸共聚物(HA-FA-Pg)的技术平台在药物递送系统开发中的潜力,HA-FA-Pg衍生物的炔丙基通过生物相容性六乙二醇(HEG)间隔基与油酸(OA)或硬脂酸(SA)残基结合。通过动态光散射(DLS)和透射电子显微镜(TEM)证实,所设计的材料(即 或 )在水性环境中呈现出明确的聚集特征,形成纳米聚集体系统。事实上,由于聚合物主链中存在亲水性部分(如透明质酸)和侧链中的疏水性部分, 和 衍生物具有在水中形成自组装的细胞相容性纳米结构聚集体的特性。此外,所设计的材料与活细胞相互作用,表现出高度的细胞相容性。通过将奥氮平物理包封到两种聚合物系统中,评估了纳米系统负载药理活性分子的潜在能力。药物负载评估表明,纳米颗粒能够掺入大量奥氮平,同时提高药物溶解度、释放曲线和细胞相容性。