Polymeric nanoparticles produced by electrohydrodynamic atomisation for the passive delivery of imatinib

IF 4.4 2区医学 Q1 PHARMACOLOGY & PHARMACY European Journal of Pharmaceutics and Biopharmaceutics Pub Date : 2024-07-14 DOI:10.1016/j.ejpb.2024.114412

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Abstract

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.

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利用电流体动力雾化技术生产的聚合物纳米颗粒，用于被动输送伊马替尼。

伊马替尼是一种化疗药物，已知全身用药会产生严重的副作用。将伊马替尼封装在共聚物聚乳酸-共羟基乙酸（PLGA）纳米颗粒（NPs）中可实现靶向给药。在这项研究中，利用电流体动力雾化技术将伊马替尼封装在 PLGA 50:50 和 PLGA 75:25 的 NPs 中。生成的颗粒均为球形，表面光滑，粒度分布为 455±115 nm（PLGA 50:50）和 363±147 nm（PLGA 75:25）。结果表明，伊马替尼的包封率高于 75%，并提高了负载 NPs 的 zeta 电位。伊马替尼的释放在最初的 12 小时内有一个初始爆发期，不同的持续释放率高达 70%。还在 A549 细胞上研究了这两种伊马替尼负载 NPs 对细胞活力的影响及其细胞摄取情况，其抗增殖效果与用游离药物处理的细胞相当。最后，罗丹明-B 载体 NP 处理的细胞证明了细胞对 NPs 的摄取。

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来源期刊

European Journal of Pharmaceutics and Biopharmaceutics 医学-药学

CiteScore

8.80

自引率

4.10%

发文量

211

审稿时长

36 days

期刊介绍： The European Journal of Pharmaceutics and Biopharmaceutics provides a medium for the publication of novel, innovative and hypothesis-driven research from the areas of Pharmaceutics and Biopharmaceutics. Topics covered include for example: Design and development of drug delivery systems for pharmaceuticals and biopharmaceuticals (small molecules, proteins, nucleic acids) Aspects of manufacturing process design Biomedical aspects of drug product design Strategies and formulations for controlled drug transport across biological barriers Physicochemical aspects of drug product development Novel excipients for drug product design Drug delivery and controlled release systems for systemic and local applications Nanomaterials for therapeutic and diagnostic purposes Advanced therapy medicinal products Medical devices supporting a distinct pharmacological effect.