Facile synthesis of interpenetrating polymeric nexus for controlled drug delivery of 5-fluorouracil (5-FU)

IF 3.1 3区 化学 Q2 POLYMER SCIENCE
Maria Malook, Asif Mahmood, Hira Ijaz, Rai Muhammad Sarfraz, Muhammad Rauf Akram, Bilal Haroon, Zulcaif Ahmad, Sadaf Ayub, Faisal Gulzar
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引用次数: 0

Abstract

The purpose of the current research study was to formulate and evaluate a fenugreek (FG) and agarose (AG) base hydrogel exploiting pH-responsive attributes and colon targeting of 5-fluorouracil (5-FU). A novel 5-FU loaded fenugreek (FG) and agarose (AG) base hydrogel was formulated via free radical polymerization by employing N’, N’methylene bisacrylamide (MBA) as a crosslinker and methacrylic acid as a monomer. The influence of substrate concentrations (FG, AG, MBA, and MAA) was studied on the swelling index, sol–gel fraction, and drug release rate (%). It was also evaluated that as the concentration of fenugreek and agarose increases, drug release increases to 94.35 ± 0.34 (%) at pH 7.4 and 13.34 ± 0.34 (%) at pH 1.2. However, an increase in MAA concentration further leads to an increase in swelling, 95.87 ± 0.23 at pH 7.4 and 14.35 ± 0.74 at pH 1.2. Moreover, MBA concentration could significantly and directly influence the swelling of hydrogels owing to the variation of crosslinking density. An increase in MBA concentration results in a significant decrease in swelling. Fourier transform infrared spectroscopy (FTIR) depicted the grafting of polymers (FG and AG) and monomers (MAA). Thermal behavior showed that the formulated nexus protects the drug and substrate from degradation. The X-ray diffraction analysis (XRD) revealed that the entrapment of the drug within the nexus mimicked its crystalline behavior. The scanning electron microscope (SEM) elucidates the porous, rough, irregular, and asymmetric nature of the nexus. Toxicity studies showed that the best-selected optimized formulated nexus (F9) is biocompatible, non-toxic, and promising for targeted delivery of 5-FU for curing colorectal cancer.

Graphical Abstract

Abstract Image

用于控制 5-氟尿嘧啶 (5-FU) 给药的互穿聚合物结合物的简便合成
本研究旨在配制和评估一种利用 pH 值响应特性和 5-氟尿嘧啶(5-FU)结肠靶向性的葫芦巴(FG)和琼脂糖(AG)基水凝胶。以 N',N'亚甲基双丙烯酰胺(MBA)为交联剂,甲基丙烯酸为单体,通过自由基聚合配制了一种新型 5-FU 负载葫芦巴(FG)和琼脂糖(AG)基水凝胶。研究了基质浓度(FG、AG、MBA 和 MAA)对溶胀指数、溶胶-凝胶部分和药物释放率(%)的影响。评估还发现,随着葫芦巴和琼脂糖浓度的增加,药物释放率在 pH 值为 7.4 时增加到 94.35 ± 0.34(%),在 pH 值为 1.2 时增加到 13.34 ± 0.34(%)。然而,MAA 浓度的增加会进一步导致溶胀增加,pH 值为 7.4 时为 95.87 ± 0.23,pH 值为 1.2 时为 14.35 ± 0.74。此外,由于交联密度的变化,MBA 的浓度也会对水凝胶的溶胀产生重大而直接的影响。MBA 浓度的增加会导致溶胀度的显著降低。傅立叶变换红外光谱(FTIR)显示了聚合物(FG 和 AG)和单体(MAA)的接枝情况。热行为表明,配制的结合物能保护药物和基质不被降解。X 射线衍射分析(XRD)显示,药物在胶结物中的嵌入模拟了其结晶行为。扫描电子显微镜(SEM)阐明了结合物多孔、粗糙、不规则和不对称的性质。毒性研究表明,最佳选择的优化配制结合物(F9)具有生物相容性、无毒性,有望用于治疗结直肠癌的 5-FU 靶向给药。
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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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