Universidad Nacional de Quilmes, Departamento de Ciencia y Tecnología, Laboratorio de Bio-Nanotecnología, Bernal, Buenos Aires, Argentina; Grupo de Biología Estructural y Biotecnología (GBEyB), IMBICE (CONICET CCT-La Plata), Buenos Aires, Argentina.
Universidad Nacional de Quilmes, Departamento de Ciencia y Tecnología, Laboratorio de Bio-Nanotecnología, Bernal, Buenos Aires, Argentina; Grupo de Biología Estructural y Biotecnología (GBEyB), IMBICE (CONICET CCT-La Plata), Buenos Aires, Argentina.
Chem Phys Lipids. 2020 Sep;231:104936. doi: 10.1016/j.chemphyslip.2020.104936. Epub 2020 Jun 24.
In the present work, we obtained polymeric diacetylene liposomes that can associate N-Acetyl-l-Cysteine (NAC), a broad spectrum mucolytic. The reason for studying these formulations is that they could be applied in the future as NAC delivery systems, with a possible dose reduction but maintaining its effect. Liposomes used herein are obtained by a photopolymerization reaction, thus gaining stability and rigidity. Lipids belonging to lung surfactant were added in different ratios to the formulations in order to maximize its possible interaction with the lung tissue. Because of lipopolymer stability, the oral or nasal route could be appropriated. This formulation could efficiently transport NAC to exert its mucolytic activity and help in diseases such as cystic fibrosis, which has abnormal mucus production. Also, this type of treatment could be useful in other types of diseases, interacting with the mucus layer and making the lung tissue more permeable to other therapies. Formulations so obtained presented high levels of polymerization. Also, they present small hollow fibers structures with a high number of polymeric units. These types of arrangements could present advantages in the field of drug delivery, giving the possibility of a controlled release. Lipopolymers with lipids from lung surfactant associated with NAC are promising complexes in order to treat not only respiratory illnesses. The stability of the formulation would allow its inoculation through other routes such as the oral one, helping the reposition of NAC as an antioxidant drug. Finally, these formulations are non-toxic and easy to produce.
在本工作中，我们获得了能够与 N-乙酰-L-半胱氨酸（NAC）结合的聚合二乙炔脂质体，NAC 是一种广谱黏液溶解剂。研究这些制剂的原因是它们将来可能被用作 NAC 递送系统，可以减少剂量但保持其效果。本文中使用的脂质体通过光聚合反应获得，从而获得稳定性和刚性。将属于肺表面活性剂的脂质以不同的比例添加到制剂中，以最大限度地提高其与肺组织的可能相互作用。由于脂质体的稳定性，可以通过口服或鼻内途径给药。这种制剂可以有效地输送 NAC 以发挥其黏液溶解活性，并有助于囊性纤维化等疾病，这些疾病的黏液产生异常。此外，这种类型的治疗在其他类型的疾病中也可能有用，与黏液层相互作用，使肺组织对其他治疗更具通透性。所得到的制剂具有高聚合水平。此外，它们还呈现出具有高分子量的小空心纤维结构。这些类型的排列在药物递送领域可能具有优势，可以实现控制释放。与肺表面活性剂的脂质结合的 NAC 脂质体具有很大的前景，不仅可以用于治疗呼吸系统疾病。该制剂的稳定性允许通过其他途径（如口服途径）接种，有助于将 NAC 重新定位为抗氧化药物。最后，这些制剂无毒且易于生产。
