QbD-based co-loading of paclitaxel and imatinib mesylate by protamine-coated PLGA nanoparticles effective on breast cancer cells.

Nanomedicine (London, England) Pub Date : 2024-01-01 Epub Date: 2024-06-27 DOI:10.1080/17435889.2024.2353557
Neha Laxane, Khushwant S Yadav
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Abstract

Aim: Paclitaxel and imatinib mesylate are drugs used in the treatment of breast cancer. Conventional drug-delivery systems have limitations in the effective treatment of breast cancer using the drugs.Materials & methods: Combination index studies were used to identify the optimum ratio of both drugs showing maximum synergistic effect. Using a systematic quality-by-design approach, protamine-coated PLGA nanoparticles co-loaded with paclitaxel and imatinib mesylate were formulated. Further characterization and cell line evaluations were performed.Results: Encapsulation efficiency obtained was 92.54% for paclitaxel and 75.12% for imatinib mesylate. A sustained (24 h) and controlled zero-order drug release was obtained.Conclusion: Formulated nanoparticles had a low IC50 value and enhanced cellular uptake.

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基于 QbD 的紫杉醇和甲磺酸伊马替尼共载原胺包覆的 PLGA 纳米颗粒对乳腺癌细胞有效。
目的:紫杉醇和甲磺酸伊马替尼是治疗乳腺癌的药物。传统的给药系统在使用这两种药物有效治疗乳腺癌方面存在局限性。材料和方法:采用组合指数研究来确定两种药物的最佳比例,以显示最大的协同效应。采用系统化的质量控制设计方法,配制出了紫杉醇和甲磺酸伊马替尼联合负载的原胺包衣聚乳酸乙二醛(PLGA)纳米颗粒。进一步的表征和细胞系评估也已完成。结果显示紫杉醇的封装效率为 92.54%,甲磺酸伊马替尼的封装效率为 75.12%。获得了持续(24 小时)、可控的零阶药物释放。结论配制的纳米颗粒具有较低的 IC50 值和较高的细胞吸收率。
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