将牛血清白蛋白纳米颗粒作为输送 10H-2,7-二氮吩噻嗪的拟议药物制剂

IF 2.7 4区 化学 Q2 CHEMISTRY, INORGANIC & NUCLEAR Journal of Cluster Science Pub Date : 2024-07-28 DOI:10.1007/s10876-024-02666-1
Karolina Kulig, Beata Morak-Młodawska, Małgorzata Jeleń, Magdalena Ziąbka, Aleksandra Owczarzy, Wojciech Rogóż, Małgorzata Maciążek-Jurczyk
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引用次数: 0

摘要

合成新化合物和纳米颗粒是规避耐药性的众多尝试之一。白蛋白纳米粒子是一种生物相容性药物载体,能够在不改变的情况下加入药物。10H-2,7-二氮吩噻嗪(2,7-DAPT)是一种新的吩噻嗪衍生物,具有抗癌、免疫调节和抗炎活性,同时对正常脾细胞的细胞毒性较低。迄今为止,2,7-DAPT 的给药途径尚未被提出,因此本研究的新颖之处在于合成含有尚未用于临床的活性成分的纳米颗粒。这项研究的目的是通过脱溶法将 2,7-DAPT 包囊到牛血清白蛋白(BSA)纳米颗粒中。这项研究还辅以 2,7-DAPT的光谱研究、尺寸和形态测量以及在 pH 值为 7.4 和 5.6 时的释放分析。2,7-DAPT 是一种在溶液中具有高稳定性的化合物,在紫外可见光范围内具有吸收能力。根据扫描电子显微镜的结果,纳米颗粒的尺寸在 204 纳米左右摆动。2,7- DAPT 从纳米颗粒中的释放具有不同的释放机制,这些机制取决于释放缓冲液的 pH 值。上述结果表明所获得的纳米颗粒具有潜在的用途。由于缺乏对含有这种物质的纳米颗粒的研究,今后需要进行更详细的分析。
本文章由计算机程序翻译,如有差异,请以英文原文为准。

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Bovine Serum Albumin Nanoparticles as a Proposed Drug Formulation for the Delivery of 10H-2,7-diazaphenothiazine

The synthesis of new compounds and nanoparticles is one of many attempts to circumvent the drug resistance. Albumin nanoparticles are biocompatible drug carriers with an ability to incorporate drugs without modifications. 10H-2,7-diazphenothiazine (2,7-DAPT) is a newly phenothiazine derivative with an anticancer, immunomodulatory and anti-inflammatory activity with a low cytotoxicity toward normal splenocytes at the same time. Up to now, no administration route for 2,7-DAPT has been proposed, so the novelty of the study is synthesis of nanoparticles containing an active ingredient not yet used in the clinic. The aim of the study was to encapsulate 2,7-DAPT into bovine serum albumin (BSA) nanoparticles by desolvation method. This study was supplemented with spectroscopic studies of 2,7-DAPT, size and morphology measurements as well as release analysis at pH 7.4 and 5.6. 2,7-DAPT is a compound with high stability in solution and an ability to absorb at UV-Vis range. Based on the results of scanning electron microscopy, nanoparticles size oscillates around the value of 204 nm. The release of 2,7- DAPT from the nanoparticles was characterized by different mechanisms of release, which were dependent on the pH of the release buffer. The above results indicate the potential usefulness of the obtained nanoparticles. Due to the lack of studies of nanoparticles containing this substance, more detailed future analyses are required.

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来源期刊
Journal of Cluster Science
Journal of Cluster Science 化学-无机化学与核化学
CiteScore
6.70
自引率
0.00%
发文量
166
审稿时长
3 months
期刊介绍: The journal publishes the following types of papers: (a) original and important research; (b) authoritative comprehensive reviews or short overviews of topics of current interest; (c) brief but urgent communications on new significant research; and (d) commentaries intended to foster the exchange of innovative or provocative ideas, and to encourage dialogue, amongst researchers working in different cluster disciplines.
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