Synthesis and Characterization of Acrylamide/Acrylic Acid Co-Polymers and Glutaraldehyde Crosslinked pH-Sensitive Hydrogels

Gels

Attalla F. El-kott¹  Roua S. Baty²  Md. Habibur Rahman³  Mohamed Kamel⁴  Mohamed M. Abdel-Daim⁵  Asif Nawaz⁶  Muhammad Safdar⁶  Munir Ahmad Khan⁶  Muhammad Akhlaq⁶  Simona G. Bungau⁷  Pijush Paul⁸  Md. Kamal Hossain⁹  Abul Kalam Azad^1,10 

[1] Biology Department, Faculty of Science, King Khalid University, P.O. Box 9004, Abha 61421, Saudi Arabia;Department of Biotechnology, College of Science, Taif University, P.O. Box 11099, Taif 21944, Saudi Arabia;Department of Global Medical Science, Wonju College of Medicine, Yonsei University, Wonju 26426, Gangwon-do, Korea;Department of Medicine and Infectious Diseases, Faculty of Veterinary Medicine, Cairo University, Giza 12211, Egypt;Department of Pharmaceutical Sciences, Batterjee Medical College, P.O. Box 6231, Jeddah 21442, Saudi Arabia;Department of Pharmaceutics, Faculty of Pharmacy, Gomal University, Dera Ismail Khan 29050, Pakistan;Department of Pharmacy, Faculty of Medicine and Pharmacy, University of Oradea, 410087 Oradea, Romania;Department of Pharmacy, Gono Bishwabidyalay, Mirzanagar, Savar, Dhaka 1344, Bangladesh;Institute of Health and Sports, Victoria University, Melbourne 3011, Australia;Pharmaceutical Technology Unit, Faculty of Pharmacy, AIMST University, Bedong 08100, Kedah, Malaysia;

关键词: hydrogels;    pH-sensitive;    colon drug delivery;    acrylamide;    acrylic acid;    glutaraldehyde;   

DOI  :  10.3390/gels8010047

来源: DOAJ

【 摘 要 】

This project aims to synthesize and characterize the pH-sensitive controlled release of 5-fluorouracil (5-FU) loaded hydrogels (5-FULH) by polymerization of acrylamide (AM) and acrylic acid (AA) in the presence of glutaraldehyde (GA) as a crosslinker with ammonium persulphate as an initiator. The formulation’s code is named according to acrylamide (A1, A2, A3), acrylic acid (B1, B2, B3) and glutaraldehyde (C1, C2, C3). The optimized formulations were exposed to various physicochemical tests, namely swelling, diffusion, porosity, sol gel analysis, and attenuated total reflection-Fourier transform infrared (ATR-FTIR). These 5-FULH were subjected to kinetic models for drug release data. The 5-FU were shown to be soluble in distilled water and phosphate buffer media at pH 7.4, and sparingly soluble in an acidic media at pH 1.2. The ATR-FTIR data confirmed that the 5-FU have no interaction with other ingredients. The lowest dynamic (0.98 ± 0.04% to 1.90 ± 0.03%; 1.65 ± 0.01% to 6.88 ± 0.03%) and equilibrium swelling (1.85 ± 0.01% to 6.68 ± 0.03%; 10.12 ± 0.02% to 27.89 ± 0.03%) of formulations was observed at pH 1.2, whereas the higher dynamic (4.33 ± 0.04% to 10.21 ± 0.01%) and equilibrium swelling (22.25 ± 0.03% to 55.48 ± 0.04%) was recorded at pH 7.4. These findings clearly indicated that the synthesized 5-FULH have potential swelling characteristics in pH 6.8 that will enhance the drug’s release in the same pH medium. The porosity values of formulated 5-FULH range from 34% to 62% with different weight ratios of AM, AA, and GA. The gel fractions data showed variations ranging from 74 ± 0.4% (A1) to 94 ± 0.2% (B3). However, formulation A1 reported the highest 24 ± 0.1% and B3 the lowest 09 ± 0.3% sol fractions rate among the formulations. Around 20% drug release from the 5-FULH was found at 1 h in an acidic media (pH1.2), whereas >65% of drug release (pH7.4) was observed at around 25 h. These findings concluded that GA crosslinked 5-FU loaded AM and AA based hydrogels would be a potential pH-sensitive oral controlled colon drug delivery carrier.

【 授权许可】

Unknown