提高药物溶解度的方法:非洛地平聚合物纳米粒子的制造、表征和安全性评估

IF 3.1 3区 化学 Q2 POLYMER SCIENCE Polymer Bulletin Pub Date : 2024-08-28 DOI:10.1007/s00289-024-05458-9
Ume Ruqia Tulain, Alia Erum, Bushra Maryam,  Sidra, Nadia Shamshad Malik, Nariman Shahid, Abdul Malik, Muhammad Zubair Malik
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引用次数: 0

摘要

本研究采用纳米沉淀法制备了负载非洛地平的纳米颗粒,以榅桲籽粘液为聚合物基质,以吐温 80 为稳定剂。利用一系列分析技术,包括动态光散射(DLS)、zeta 电位测量、傅立叶变换红外光谱(FTIR)、热分析、X 射线衍射(XRD)和扫描电子显微镜(SEM),对纳米颗粒进行了全面的表征。非洛地平纳米颗粒显示出无定形结构,其中 FEL 4 配方的包埋效率最高,达到 67.68%。该配方的平均粒径为 675 ± 2.04 nm,zeta 电位为 - 31.7 ± 1.34 mV。饱和溶解度测试表明,与纯非洛地平相比,纳米颗粒的水溶性显著提高。此外,体外药物释放研究表明,非洛地平在磷酸盐缓冲液中可持续释放 24 小时。急性口服毒性评估证实,非洛地平纳米颗粒没有表现出任何毒性迹象。总之,这项研究表明,成功制备出以榅桲籽粘液为基础的非洛地平纳米颗粒是一种很有前景的方法,可提高药物的溶解度,实现药物的持续释放,且无明显毒性。
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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An approach to enhance drug solubility: fabrication, characterization, and safety evaluation of Felodipine polymeric nanoparticles

In this study, Felodipine-loaded nanoparticles were prepared using the nanoprecipitation method, with quince seed mucilage serving as the polymer matrix and Tween 80 utilized as a stabilizing agent. The nanoparticles were thoroughly characterized using a range of analytical techniques, including dynamic light scattering (DLS), zeta potential measurement, Fourier-transform infrared spectroscopy (FTIR), thermal analysis, X-ray diffraction (XRD), and scanning electron microscopy (SEM). The Felodipine nanoparticles displayed an amorphous structure, with formulation FEL 4 achieving the highest entrapment efficiency of 67.68%. This formulation also had an average particle size of 675 ± 2.04 nm and a zeta potential of − 31.7 ± 1.34 mV. Saturation solubility tests revealed a significant enhancement in water solubility for the nanoparticles compared to pure Felodipine. Additionally, in vitro drug release studies demonstrated a sustained release profile over 24 h in phosphate buffer. Acute oral toxicity evaluations confirmed that the Felodipine nanoparticles did not exhibit any signs of toxicity. Overall, this study showed the successful fabrication of quince seed mucilage-based Felodipine-loaded nanoparticles as a promising approach to enhance solubility and achieve sustained drug release, with no evident toxicity.

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来源期刊
Polymer Bulletin
Polymer Bulletin 化学-高分子科学
CiteScore
6.00
自引率
6.20%
发文量
0
审稿时长
5.5 months
期刊介绍: "Polymer Bulletin" is a comprehensive academic journal on polymer science founded in 1988. It was founded under the initiative of the late Mr. Wang Baoren, a famous Chinese chemist and educator. This journal is co-sponsored by the Chinese Chemical Society, the Institute of Chemistry, and the Chinese Academy of Sciences and is supervised by the China Association for Science and Technology. It is a core journal and is publicly distributed at home and abroad. "Polymer Bulletin" is a monthly magazine with multiple columns, including a project application guide, outlook, review, research papers, highlight reviews, polymer education and teaching, information sharing, interviews, polymer science popularization, etc. The journal is included in the CSCD Chinese Science Citation Database. It serves as the source journal for Chinese scientific and technological paper statistics and the source journal of Peking University's "Overview of Chinese Core Journals."
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