"Development, optimization, and characterization of Eudragit-based nanoparticles for Dasatinib delivery".

IF 3.6 4区 医学 Q2 ENGINEERING, BIOMEDICAL Journal of Biomaterials Science, Polymer Edition Pub Date : 2024-11-19 DOI:10.1080/09205063.2024.2427489
Hemanth G, Anasuya Patil, Hariprasad Mg, Moqbel Ali Moqbel Redhwan, Sourav Guha
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Abstract

This study focused on developing and evaluating dasatinib-loaded nanoparticles (DST-NPs) using Eudragit L100 as a polymer matrix for enhanced breast cancer treatment. The optimized formulation exhibited a particle size of 202.1 ± 5.7 nm, a zeta potential of -18 ± 1.01 mV, and an entrapment efficiency of 93.11 ± 0.2%. In-vitro release studies demonstrated sustained drug release from DST-NPs, following Fickian diffusion. Pharmacokinetic studies in rats revealed higher Cmax and AUC0-t for DST-NPs compared to pure DST, indicating improved bioavailability. Tissue distribution studies showed enhanced targeting of DST-NPs, with higher concentrations in the liver and spleen. In vivo efficacy in a DMBA-induced mammary carcinoma model demonstrated that DST-NPs significantly reduced tumor volume, maintained stable body weight, and improved survival rates compared to pure DST. Hematologic analysis indicated a favorable blood profile with DST-NPs, and histopathological examinations confirmed the restoration of normal mammary gland and liver architecture. MTT assays showed higher cytotoxicity of DST-NPs against MCF-7, MDA-MB231, and 4T1 cell lines, with lower IC50 values than pure DST. Stability studies indicated that DST-NPs maintained their properties over six months at various storage conditions. These findings highlight the potential of DST-NPs as an effective nanocarrier system for cancer therapy.

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"用于达沙替尼给药的基于 Eudragit 的纳米颗粒的开发、优化和表征"。
本研究以 Eudragit L100 为聚合物基质,重点开发和评估了达沙替尼负载纳米颗粒(DST-NPs),用于增强乳腺癌治疗效果。优化配方的粒径为 202.1 ± 5.7 nm,zeta 电位为 -18 ± 1.01 mV,包埋效率为 93.11 ± 0.2%。体外释放研究表明,DST-NPs 可通过费克扩散作用持续释放药物。大鼠药代动力学研究显示,与纯 DST 相比,DST-NPs 的 Cmax 和 AUC0-t 更高,表明生物利用度有所提高。组织分布研究表明,DST-NPs 的靶向性更强,在肝脏和脾脏的浓度更高。在 DMBA 诱导的乳腺癌模型中的体内疗效表明,与纯 DST 相比,DST-NPs 能显著减少肿瘤体积,保持体重稳定,并提高存活率。血液学分析表明,DST-NPs 有助于改善血液状况;组织病理学检查证实,DST-NPs 恢复了正常的乳腺和肝脏结构。MTT 试验表明,DST-NPs 对 MCF-7、MDA-MB231 和 4T1 细胞株的细胞毒性更高,IC50 值低于纯 DST。稳定性研究表明,DST-NPs 在不同的储存条件下可保持 6 个月的特性。这些发现凸显了 DST-NPs 作为一种有效的癌症治疗纳米载体系统的潜力。
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来源期刊
Journal of Biomaterials Science, Polymer Edition
Journal of Biomaterials Science, Polymer Edition 工程技术-材料科学:生物材料
CiteScore
7.10
自引率
5.60%
发文量
117
审稿时长
1.5 months
期刊介绍: The Journal of Biomaterials Science, Polymer Edition publishes fundamental research on the properties of polymeric biomaterials and the mechanisms of interaction between such biomaterials and living organisms, with special emphasis on the molecular and cellular levels. The scope of the journal includes polymers for drug delivery, tissue engineering, large molecules in living organisms like DNA, proteins and more. As such, the Journal of Biomaterials Science, Polymer Edition combines biomaterials applications in biomedical, pharmaceutical and biological fields.
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