厄洛替尼治疗乳腺癌的叶酸靶向纳米脂系统的开发和体内生物分布。

Nanomedicine (London, England) Pub Date : 2025-07-01 Epub Date: 2025-05-26 DOI:10.1080/17435889.2025.2508135
Bharti Mangla, Tabish Pathan, Pankaj Kumar, Geeta Aggarwal
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引用次数: 0

摘要

目的:研制叶酸靶向纳米脂载体系统(fa - ert - nnlcs),研究其体内口服生物分布及其吸收机制。材料与方法:通过吡啶和EDC化学偶联叶酸。采用高压均质法制备FA-ERT-NLCs,并通过设计专家软件对参数进行优化。FA-ERT-NLCs通过体外表征、体外和体内生物分布研究进行评估。此外,本研究采用雌性Wistar大鼠。结果:在带负电荷表面的纳米范围(182.34 nm)内发现了靶向NLCs, PDI分别为-16.2 mV和0.203。测定其叶酸含量为71.33%。在大鼠肠内发现ERT和FC-ERT-NLCs的深度分别为20µm和80.2µm。所研制的制剂对MCF-7细胞系有效。ERT的IC50值为526.2µg/mL, fc -ERT- nlc的IC50值为333.7µg/mL。FA-ERT-NLCs经肠道淋巴系统吸收。结论:本研究为有效、安全的乳腺癌治疗提供了有希望的靶向策略。
本文章由计算机程序翻译,如有差异,请以英文原文为准。
Development and in vivo biodistribution of folate-targeted nanolipid system for erlotinib in breast cancer treatment.

Aim: The aim of the study was to develop folate targeted nanolipid carrier system (FA-ERT-NLCs) and study its in vivo oral biodistribution study for its absorption mechanism.

Materials & methods: Folic acid was conjugated through pyridine and EDC chemistry. FA-ERT-NLCs was developed by high-pressure homogenization and parameters were optimized through design expert software. FA-ERT-NLCs were evaluated through in vitro characterization, Ex vivo and in vivo biodistribution studies. Moreover, female Wistar rats were used in this study.

Results: Findings showed that targeted NLCs were found in nanometric range (182.34 nm) with negatively charge surface and PDI was found to be -16.2 mV and 0.203. The folate content in the conjugate was measured and found to be 71.33%. The depth of ERT and FC-ERT-NLCs was found to be 20 µm and 80.2 µm in rat intestine. Developed formulation was effective against MCF-7 cell lines. The IC50 values were found to be 526.2 µg/mL for ERT and 333.7 µg/mL for FC-ERT-NLCs. FA-ERT-NLCs are absorbed through intestine by lymphatic system.

Conclusion: This study showed a promising targeted strategy for effective and safer breast cancer treatment.

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