Laidmäe Ivo, Meos Andres, Kjærvik Irja Alainezhad, Ingebrigtsen Sveinung G, Škalko-Basnet Nataša, Kirsimäe Kalle, Romann Tavo, Joost Urmas, Kisand Vambola, Kogermann Karin
Institute of Pharmacy, Faculty of Medicine, University of Tartu, Nooruse 1, 50411 Tartu, Estonia.
Department of Immunology, University of Tartu, Ravila 19, 50411 Tartu, Estonia.
Pharmaceutics. 2021 Oct 20;13(11):1742. doi: 10.3390/pharmaceutics13111742.
The hydration of phospholipids, electrospun into polymeric nanofibers and used as templates for liposome formation, offers pharmaceutical advantages as it avoids the storage of liposomes as aqueous dispersions. The objective of the present study was to electrospin and characterize amphiphilic nanofibers as templates for the preparation of antibiotic-loaded liposomes and compare this method with the conventional film-hydration method followed by extrusion. The comparison was based on particle size, encapsulation efficiency and drug-release behavior. Chloramphenicol (CAM) was used at different concentrations as a model antibacterial drug. Phosphatidylcoline (PC) with polyvinylpyrrolidone (PVP), using ethanol as a solvent, was found to be successful in fabricating the amphiphilic composite drug-loaded nanofibers as well as liposomes with both methods. The characterization of the nanofiber templates revealed that fiber diameter did not affect the liposome size. According to the optical microscopy results, the immediate hydration of phospholipids deposited on the amphiphilic nanofibers occurred within a few seconds, resulting in the formation of liposomes in water dispersions. The liposomes appeared to aggregate more readily in the concentrated than in the diluted solutions. The drug encapsulation efficiency for the fiber-hydrated liposomes varied between 14.9 and 28.1% and, for film-hydrated liposomes, between 22.0 and 77.1%, depending on the CAM concentrations and additional extrusion steps. The nanofiber hydration method was faster, as less steps were required for the in-situ liposome preparation than in the film-hydration method. The liposomes obtained using nanofiber hydration were smaller and more homogeneous than the conventional liposomes, but less drug was encapsulated.
将磷脂水合后静电纺丝成聚合物纳米纤维，并用作脂质体形成的模板，具有药学优势，因为它避免了将脂质体储存为水分散体。本研究的目的是静电纺丝并表征两亲性纳米纤维作为制备载抗生素脂质体的模板，并将该方法与随后进行挤压的传统薄膜水化法进行比较。比较基于粒径、包封效率和药物释放行为。使用不同浓度的氯霉素（CAM）作为模型抗菌药物。发现磷脂酰胆碱（PC）与聚乙烯吡咯烷酮（PVP），以乙醇作为溶剂，两种方法都成功制备了两亲性复合载药纳米纤维以及脂质体。纳米纤维模板的表征表明纤维直径不影响脂质体大小。根据光学显微镜结果，沉积在两亲性纳米纤维上的磷脂在几秒钟内立即水合，导致在水分散体中形成脂质体。脂质体在浓缩溶液中似乎比在稀释溶液中更容易聚集。根据CAM浓度和额外的挤压步骤，纤维水合脂质体的药物包封效率在14.9%至28.1%之间，薄膜水合脂质体的药物包封效率在22.0%至77.1%之间。纳米纤维水合法更快，因为原位制备脂质体所需的步骤比薄膜水合法少。使用纳米纤维水合获得的脂质体比传统脂质体更小且更均匀，但包封的药物更少。
