School of Pharmacy, University College London, London, United Kingdom.
National Pulmonary Hypertension Service, Royal Free London NHS Foundation Trust, Pond Street, London, NW3 2QG, United Kingdom.
Eur J Pharm Biopharm. 2024 Sep;202:114412. doi: 10.1016/j.ejpb.2024.114412. Epub 2024 Jul 14.
Imatinib is a chemotherapeutic agent known to cause severe side effects when administrated systemically. Encapsulating imatinib in co-polymer poly(lactic-co-glycolic acid) (PLGA) nanoparticles (NPs) offers a targeted drug delivery. In this work, PLGA 50:50 and PLGA 75:25 NPs encapsulated imatinib using the electrohydrodynamic atomisation technique. All particles generated were spherical with a smooth surface with a size distribution of 455±115 nm (PLGA 50:50) and 363±147 nm (PLGA 75:25). Encapsulation of imatinib was shown to be higher than 75 % and was shown to increase the zeta potential of the loaded NPs. The release of imatinib showed an initial burst in the first 12 h, followed by different sustained releases with up to 70 %. Both types of imatinib-loaded NPs' effect on cell viability and their cellular uptake were also studied on A549 cells, and the antiproliferative effect was comparable to that of cells treated with free drugs. Finally, Rhodamine-B-loaded NP-treated cells demonstrated the cellular uptake of NPs.
伊马替尼是一种化疗药物，已知全身给药会引起严重的副作用。将伊马替尼包封在共聚物聚（乳酸-共-乙醇酸）（PLGA）纳米颗粒（NPs）中提供了靶向药物递送。在这项工作中，使用电动力学雾化技术将 PLGA 50:50 和 PLGA 75:25 NPs 包封伊马替尼。所有生成的颗粒均为球形，表面光滑，粒径分布分别为 455±115nm（PLGA 50:50）和 363±147nm（PLGA 75:25）。伊马替尼的包封率高于 75%，并显示负载 NPs 的 Zeta 电位增加。伊马替尼的释放显示出最初在 12 小时内的初始突释，随后是长达 70%的不同持续释放。还研究了两种载有伊马替尼的 NPs 对 A549 细胞的细胞活力和细胞摄取的影响，其增殖抑制作用与用游离药物处理的细胞相当。最后，用 Rhodamine-B 负载的 NP 处理的细胞证明了 NPs 的细胞摄取。
