氯二胺[N，N'-双（水杨基）-1,2-苯二胺]铁的潜力评估（III）：通过脂质纳米载体的递送探索。

IF 4.7 3区医学 Q1 PHARMACOLOGY & PHARMACY

European Journal of Pharmaceutical Sciences Pub Date : 2025-07-18 DOI:10.1016/j.ejps.2025.107206

Marlene Ramona Schmidt , Astrid Dagmar Bernkop-Schnürch , Daniel Stengel , Magnus Andre Kiechle , Khush Bakhat Afzal , Anna Seybold , Martin Hermann , Brigitte Kircher , Andreas Bernkop-Schnürch

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引用次数: 0

摘要

目的：本研究概述了一种用于给药氯ido[N，N'-双（水杨柳二烯）-1,2-苯二胺]-铁（III） salophene -指定铁（III） salophene （Fe³⁺SP）的创新递送系统的开发。方法：采用傅里叶红外光谱（FTIR）验证Fe + SP的身份，并采用高效液相色谱（HPLC）测定其亲脂性（log P）。然后将Fe³+ SP掺入脂基纳米载体（lbnc）中，脂质基质为辛酸/癸酸甘油三酯(45.4%；V / V)，磷脂酰胆碱(36.4%；甲醇和苯甲醇(18.2%；V / V)作为溶剂。通过MTT法研究了不同乳腺细胞系的代谢活性，并通过共聚焦激光扫描显微镜分析了不同染料对细胞摄取的影响。结果：Fe3+ sp配合物的对数P值为1.8，证实了Fe3+ sp配合物具有足够的亲脂性，可以并入脂基纳米载体中。超声处理后，空白和Fe³+ SP lbnc的粒径从1000 nm减小到200 nm左右，颗粒均匀度从1.0提高到0.2左右。不同的稳定性研究表明，在不同的缓冲系统（150-230 nm）中，液滴大小在14天内保持一致，均匀的颗粒分布（~ 0.2）证实了生理介质在48小时内的稳定性。TEM分析显示，Fe³⁺SP保持了均匀的形态，增强了稳定性，导致颗粒大小和形状一致，促进细胞吸收。与DMSO中的Fe + SP相比，负载lbnc的配方在相似的细胞摄取下对癌细胞系的效果高5倍，表明更高的疗效。结论：这些发现表明，lbnc为Fe + SP的口服递送提供了一个有前景的平台，与传统的递送系统相比具有显著的优势。

本文章由计算机程序翻译，如有差异，请以英文原文为准。

Assessing the potential of chlorido[N,N'-bis(salicylidene)-1,2-phenylenediamine]iron(III): Exploring delivery through lipid-based nanocarriers

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Assessing the potential of chlorido[N,N'-bis(salicylidene)-1,2-phenylenediamine]iron(III): Exploring delivery through lipid-based nanocarriers

Aim

This research outlines the development of an innovative delivery system for administration of chlorido[N,N'-bis(salicylidene)-1,2-phenylenediamine]-iron(III) salophene – designated Iron(III) Salophene (Fe³⁺SP).

Methodology

The identity of Fe³⁺SP was confirmed using FTIR, and its lipophilicity (log P) was quantified by HPLC. Fe³⁺SP was then incorporated into lipid-based nanocarriers (LBNCs) with a lipid matrix of triglycerides of caprylic/capric acid (45.4 %; v/v), phosphatidylcholine (36.4 %; m/v) and benzyl alcohol (18.2 %; v/v) as solvent. Metabolic activity was investigated via the MTT assay on various cell lines, and cellular uptake was analyzed by confocal laser scanning microscopy using different dyes.

Results

The log P value of 1.8 for the Fe³⁺SP-complex confirmed sufficient lipophilicity for incorporation into lipid-based nanocarriers. Ultrasonic treatment significantly reduced particle size from 1000 nm to about 200 nm and improved particle uniformity from 1.0 to about 0.2 for blank and Fe³⁺SP LBNCs. Different stability studies showed consistent droplet sizes in various buffer systems (150–230 nm) over 14 days, and uniform particle distribution (∼0.2) confirmed stability in physiological media over 48 h. TEM analysis revealed that Fe³⁺SP maintains uniform morphology and enhances stability, leading to consistent particle size and shape, promoting cellular uptake. Compared to Fe³⁺SP in DMSO, the LBNC-loaded formulation exhibited a five-fold higher effect on cancer cell lines at a similar cellular uptake, indicating higher efficacy.

Conclusion

These findings suggest that LBNCs offer a promising platform for the oral delivery of Fe³⁺SP, with significant advantages over conventional delivery systems.

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来源期刊

European Journal of Pharmaceutical Sciences 医学-药学

CiteScore

9.60

自引率

2.20%

发文量

248

审稿时长

50 days

期刊介绍： The journal publishes research articles, review articles and scientific commentaries on all aspects of the pharmaceutical sciences with emphasis on conceptual novelty and scientific quality. The Editors welcome articles in this multidisciplinary field, with a focus on topics relevant for drug discovery and development. More specifically, the Journal publishes reports on medicinal chemistry, pharmacology, drug absorption and metabolism, pharmacokinetics and pharmacodynamics, pharmaceutical and biomedical analysis, drug delivery (including gene delivery), drug targeting, pharmaceutical technology, pharmaceutical biotechnology and clinical drug evaluation. The journal will typically not give priority to manuscripts focusing primarily on organic synthesis, natural products, adaptation of analytical approaches, or discussions pertaining to drug policy making. Scientific commentaries and review articles are generally by invitation only or by consent of the Editors. Proceedings of scientific meetings may be published as special issues or supplements to the Journal.