AGH University of Science and Technology, Faculty of Materials Science and Ceramics, Al. Mickiewicza 30, 30-059 Kraków, Poland; The University of Sydney, Faculty of Pharmacy, Pharmacy Building A15, Sydney, NSW 2006, Australia.
AGH University of Science and Technology, Faculty of Materials Science and Ceramics, Al. Mickiewicza 30, 30-059 Kraków, Poland.
Mater Sci Eng C Mater Biol Appl. 2020 Jun;111:110801. doi: 10.1016/j.msec.2020.110801. Epub 2020 Mar 2.
Despite recent advancements in medicine, lung cancer still lacks an effective therapy. In the present study we have decided to combine superparamagnetic iron oxide nanoparticles (SPION) with solid lipid microparticles to develop novel, stimuli-sensitive drug carriers that increase the bioavailability of the anticancer drug (paclitaxel - PAX) through guided accumulation directly at the tumour site and controlled drug delivery. SPION and PAX-loaded microparticles (MPs) were fabricated from lauric acid (LAU) and a mixture of myristic and palmitic acids (MYR/PAL) using hot oil-in-water emulsification method. MP size, surface properties, melting temperature and magnetic mobility were evaluated along with their in vitro efficacy against malignant lung epithelial cells (A549). MPs were spherical in shape with the average particle size between 2 and 3.5 μm and responded to external magnetic field up to the distance of 15 mm. MPs were effectively internalised by the cells. Unloaded or NP-loaded MPs were cytocompatible with A549 cells, while NP + PAX-loaded MPs significantly decreased cell viability and effectively suppressed colony formation. The developed stimuli-sensitive, inhalable MPs have shown promising results as PAX carriers for controlled pulmonary delivery for the treatment of lung cancer.
尽管医学在最近取得了进步，但肺癌仍然缺乏有效的治疗方法。在本研究中，我们决定将超顺磁氧化铁纳米粒子 (SPION) 与固体脂质毫微粒结合，开发新型的、对刺激敏感的药物载体，通过在肿瘤部位的直接引导性聚集和控制药物释放，提高抗癌药物（紫杉醇-PAX）的生物利用度。使用热油-水乳化法，由月桂酸 (LAU) 和肉豆蔻酸和棕榈酸的混合物 (MYR/PAL) 制备载有 SPION 和 PAX 的毫微粒 (MP)。评估了 MP 的粒径、表面特性、熔融温度和磁迁移率，以及它们对恶性肺上皮细胞 (A549) 的体外疗效。MP 呈球形，平均粒径在 2 到 3.5 μm 之间，对外界磁场的响应距离可达 15mm。MP 能被细胞有效内化。未载药或载 NP 的 MPs 与 A549 细胞的细胞相容性良好，而 NP+PAX 载药的 MPs 则显著降低了细胞活力并有效抑制了集落形成。开发的这种对刺激敏感的、可吸入的 MPs 作为 PAX 载体，具有用于治疗肺癌的经肺控释给药的应用前景。
