Dałek Paulina, Borowik Tomasz, Reczyńska Katarzyna, Pamuła Elżbieta, Chrzanowski Wojciech, Langner Marek
Department of Biomedical Engineering, Wrocław University of Science and Technology, Wybrzeże Stanisława Wyspiańskiego 27, 51-270 Wrocław, Poland.
Lipotech Sp. Z o.o., Wadowicka 8A, 30-415 Kraków, Poland.
Langmuir. 2020 Sep 22;36(37):11138-11146. doi: 10.1021/acs.langmuir.0c02141. Epub 2020 Sep 11.
The fatty acid-based microparticles containing iron oxide nanoparticles and paclitaxel (PAX) are a viable proposition for the treatment of lung cancer. The microparticles inhaled as a dry powder can be guided to selected locations using an external magnetic field, and when accumulated there, the active compound release can be triggered by local hyperthermia. However, this general strategy requires that the active compound is released from microparticles and can reach the targeted cells before microparticles are removed. Isothermal titration calorimetry was used to demonstrate that the components of microparticles were released and transferred to albumins and lipid bilayers. The morphology of the measured particulates was studied with scanning electron microscopy and dynamic light scattering. To determine the cytotoxicity of microparticles, cell culture studies were done. It has been shown that the transfer efficiency depends predominantly on the fatty acid composition of microparticles, which, together with the active ingredient, accumulate predominantly in membrane structures after being released from microparticles and before entering the cytoplasm. The release process is sufficient; hence, paclitaxel-loaded microparticles effectively suppressed the proliferation of A549 human lung epithelial cells of malignant origin (IC values for both lauric acid-based and myristic/palmitic-based microparticles containing paclitaxel were below 0.375 μg/mL), while reference microparticles were noncytotoxic.
含有氧化铁纳米颗粒和紫杉醇（PAX）的脂肪酸基微粒是治疗肺癌的一个可行方案。以干粉形式吸入的微粒可以利用外部磁场引导至选定位置，当微粒在那里聚集时，局部热疗可触发活性化合物的释放。然而，这一总体策略要求活性化合物从微粒中释放出来，并在微粒被清除之前能够到达靶细胞。等温滴定量热法被用于证明微粒的成分被释放并转移至白蛋白和脂质双层。通过扫描电子显微镜和动态光散射研究了所测微粒的形态。为了确定微粒的细胞毒性，进行了细胞培养研究。结果表明，转移效率主要取决于微粒的脂肪酸组成，脂肪酸与活性成分一起，在从微粒释放后但进入细胞质之前，主要积聚在膜结构中。释放过程是充分的；因此，载有紫杉醇的微粒有效抑制了恶性来源的A549人肺上皮细胞的增殖（含紫杉醇的月桂酸基微粒和肉豆蔻酸/棕榈酸基微粒的IC值均低于0.375μg/mL），而对照微粒无细胞毒性。
