Visualization of the degradation of long-acting microneedles and correlation of drug release in vivo based on FRET mechanism

IF 9.4 1区 医学 Q1 ENGINEERING, BIOMEDICAL
Qingwei He , Hong Lu , Yuying Chen , Huiying Zeng , Ping Hu
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Abstract

This study introduces a live imaging technique for real-time, non-invasive monitoring of drug release from long-acting microneedles using FRET (Fluorescence Resonance Energy Transfer). Employing Cy5.5 and Cy7 as FRET pairs and levonorgestrel as the model drug, we fabricated microneedles with varying PLGA molecular weights, demonstrating distinct release profiles. The FRET-PLGA-10-MN demonstrated a rapid drug release profile, reaching nearly complete release within a two-day period, while FRET-PLGA-30-MN showed a sustained release over four days. Sensitized Emission FRET (SE-FRET) optimized the imaging process, providing a robust correlation between FRET signals and drug absorption. This method surpasses traditional pharmacokinetic studies by offering a more efficient and comprehensive analysis of microneedle release dynamics in vivo, paving the way for enhanced long-acting microneedle design and therapeutic outcomes.

Statement of significance

1. FRET technology was applied to microneedle drug delivery system for the first time, which realized real-time, quantitative and non-invasive monitoring of drug release process.
2. The long-term microneedle technique was combined with sensitized emission method, and the FRET remaining ratio was innovatively used to investigate the FRET characteristics of microneedles, and the fluorescence ratio of FRET and donor double-channel was quantitatively calculated.
3. The correlation between visual fluorescence images of FRET effect and semi-quantitative calculation results based on fluorescence intensity and drug release in vivo with drug-loaded microneedles was analyzed.

Abstract Image

基于 FRET 机制的长效微针降解可视化和体内药物释放相关性。
本研究介绍了一种利用 FRET(荧光共振能量转移)实时、无创监测长效微针药物释放的实时成像技术。我们采用 Cy5.5 和 Cy7 作为 FRET 对,以左炔诺孕酮为模型药物,制作了不同分子量的 PLGA 微针,并展示了不同的释放曲线。FRET-PLGA-10-MN 显示了快速的药物释放曲线,在两天内几乎完全释放,而 FRET-PLGA-30-MN 显示了四天的持续释放。敏化发射 FRET(SE-FRET)优化了成像过程,提供了 FRET 信号与药物吸收之间的强相关性。这种方法超越了传统的药代动力学研究,能更有效、更全面地分析微针在体内的释放动态,为提高长效微针的设计和治疗效果铺平了道路。意义声明:1. 首次将 FRET 技术应用于微针给药系统,实现了对药物释放过程的实时、定量和无创监测。2.将长期微针技术与敏化发射法相结合,创新性地利用FRET剩余比来研究微针的FRET特性,定量计算了FRET和供体双通道的荧光比。3.分析了FRET效应的直观荧光图像和基于荧光强度的半定量计算结果与药物载体微针体内药物释放的相关性。
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来源期刊
Acta Biomaterialia
Acta Biomaterialia 工程技术-材料科学:生物材料
CiteScore
16.80
自引率
3.10%
发文量
776
审稿时长
30 days
期刊介绍: Acta Biomaterialia is a monthly peer-reviewed scientific journal published by Elsevier. The journal was established in January 2005. The editor-in-chief is W.R. Wagner (University of Pittsburgh). The journal covers research in biomaterials science, including the interrelationship of biomaterial structure and function from macroscale to nanoscale. Topical coverage includes biomedical and biocompatible materials.
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上海源叶 Levonorgestrel
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