Maria Malook, Asif Mahmood, Hira Ijaz, Rai Muhammad Sarfraz, Muhammad Rauf Akram, Bilal Haroon, Zulcaif Ahmad, Sadaf Ayub, Faisal Gulzar
{"title":"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","authors":"Maria Malook, Asif Mahmood, Hira Ijaz, Rai Muhammad Sarfraz, Muhammad Rauf Akram, Bilal Haroon, Zulcaif Ahmad, Sadaf Ayub, Faisal Gulzar","doi":"10.1007/s00289-024-05477-6","DOIUrl":null,"url":null,"abstract":"<div><p>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.</p><h3>Graphical Abstract</h3><div><figure><div><div><picture><source><img></source></picture></div></div></figure></div></div>","PeriodicalId":737,"journal":{"name":"Polymer Bulletin","volume":"81 18","pages":"16635 - 16669"},"PeriodicalIF":3.1000,"publicationDate":"2024-09-06","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":"0","resultStr":"{\"title\":\"Facile synthesis of interpenetrating polymeric nexus for controlled drug delivery of 5-fluorouracil (5-FU)\",\"authors\":\"Maria Malook, Asif Mahmood, Hira Ijaz, Rai Muhammad Sarfraz, Muhammad Rauf Akram, Bilal Haroon, Zulcaif Ahmad, Sadaf Ayub, Faisal Gulzar\",\"doi\":\"10.1007/s00289-024-05477-6\",\"DOIUrl\":null,\"url\":null,\"abstract\":\"<div><p>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. 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Facile synthesis of interpenetrating polymeric nexus for controlled drug delivery of 5-fluorouracil (5-FU)
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.
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."