Abstract:In this study, poly(2-acrylamido-2-methyl-1-propane sulfonic acid-co-1-vinyl-2-pyrrolidone), P(AMPS-co-VP), hydrogels were prepared by free radical cross-linking polymerization method in deionized water at 60 • C for 24 hours with different molar percentages of AMPS and VP. In the preparation of hydrogels, ammonium persulphate (APS), N,N'-methylenebisacrylamide (NMBA) and N,N,N',N'-tetramethylethylenediamine (TEMED) were used as initiator, cross-linking agent and accelerator, respectively. NMBA was used in amo… Show more
“…This decreased swelling percentage was ascribed to the reduced porous network structure and diffusion due to increased crosslinked density. Çavuş and Çakal also reported same swelling trend by incremental rise of crosslinker 32 …”
This project was designed to develop pH responsive smart chitosan/agarose‐g‐poly (methacrylate) hydrogels using free radical polymerization for targeted delivery of Capecitabine (a prodrug of 5‐fluorouracil) for the treatment of colorectal cancer. Developed hydrogels were evaluated for drug loading efficiency, thermal stability, compatibility of components, morphology, swelling behavior, release kinetics and acute oral toxicity studies in rabbits. Moreover, pharmacokinetic parameters were also measured in healthy rabbits. Structural entanglement was confirmed via FTIR providing evidence of hydrogel formation. Loading of Capecitabine was in range from 60.35% to 62.57%. Hydrogels showed pH‐responsive behavior by providing maximum swelling of 93.84% at pH 7.4 identical to colon. Release of Capecitabine from hydrogels was in controlled pattern over a period of 36 h. Toxicity studies revealed no signs of ocular, dermal and oral toxicity providing safety evidence of hydrogels. In addition, pharmacokinetic evaluations of Capecitabine loaded hydrogels showed significant increase in plasma half‐life of 17 h and AUC of 57.65 μg.h/ml in comparison to pure Capecitabine solution. Therefore, these results strongly suggest that newly formed hydrogels are biocompatible, capable of providing sustained release at specific pH and can be employed as a cargo for colorectal delivery.
“…This decreased swelling percentage was ascribed to the reduced porous network structure and diffusion due to increased crosslinked density. Çavuş and Çakal also reported same swelling trend by incremental rise of crosslinker 32 …”
This project was designed to develop pH responsive smart chitosan/agarose‐g‐poly (methacrylate) hydrogels using free radical polymerization for targeted delivery of Capecitabine (a prodrug of 5‐fluorouracil) for the treatment of colorectal cancer. Developed hydrogels were evaluated for drug loading efficiency, thermal stability, compatibility of components, morphology, swelling behavior, release kinetics and acute oral toxicity studies in rabbits. Moreover, pharmacokinetic parameters were also measured in healthy rabbits. Structural entanglement was confirmed via FTIR providing evidence of hydrogel formation. Loading of Capecitabine was in range from 60.35% to 62.57%. Hydrogels showed pH‐responsive behavior by providing maximum swelling of 93.84% at pH 7.4 identical to colon. Release of Capecitabine from hydrogels was in controlled pattern over a period of 36 h. Toxicity studies revealed no signs of ocular, dermal and oral toxicity providing safety evidence of hydrogels. In addition, pharmacokinetic evaluations of Capecitabine loaded hydrogels showed significant increase in plasma half‐life of 17 h and AUC of 57.65 μg.h/ml in comparison to pure Capecitabine solution. Therefore, these results strongly suggest that newly formed hydrogels are biocompatible, capable of providing sustained release at specific pH and can be employed as a cargo for colorectal delivery.
Introduction:
Hydrogels are hydrophilic polymers which are cross-linked to form three-dimensional structures, which can absorb, swell and retain huge amounts
of water or aqueous fluids.
Objective:
This paper reports the preparation and characterisation of Poly(2-Acrylamido-2-Methylpropane Sulphonic Acid) (PAMPS) hydrogel with different
crosslinking intensities.
Methodology:
2-Acrylamido-2-methylpropane sulfonic acid (AMPS)
monomer was purchased from Alfa Aesar Company as reagent
grade. It was used as received (>98% purity) without any
further purification.
PAMPS hydrogel was prepared by free radical crosslinking
solution polymerization of AMPS in water at room
temperature under a nitrogen blanket in cylindrical glass tubes.
The characteristics of the obtained PAMPS hydrogel were compared with those of commercial sodium polyacrylates
hydrogel.
Results:
It was found that decreasing the crosslinker weight improved the absorbance capacity but to a limit. The suggested reasons were
discussed. The mixture showed higher absorbance rate than PAMPS, and bigger absorbance capacity than sodium polyacrylates.
Conclusion:
This paper investigates the effect of crosslinker ratio on the
swelling capacity of PAMPS. It was found that as the
crosslinking ratio decreases, the porosity of the hydrogel
increases, thus improving the swelling capacity.
Free-radical polymerization technique was adopted to fabricate a stimuli-responsive intelligent quince/mucin co-poly (methacrylate) hydrogel for the controlled delivery of acyclovir sodium. The developed hydrogel matrices were appraised using different parameters, such as drug loading (%), swelling kinetics, pH- and electrolyte-responsive swelling, and sol–gel fraction. Drug-excipient compatibility study, scanning electron microscopy, thermal analysis, powder X-ray diffraction (PXRD) analysis, in vitro drug release studies, drug release kinetics and acute oral toxicity studies were conducted. The results of drug loading revealed an acyclovir sodium loading of 63–75% in different formulations. The hydrogel discs exhibited pH-responsive swelling behavior, showing maximum swelling in a phosphate buffer with a pH of 7.4, but negligible swelling was obvious in an acidic buffer with a pH of 1.2. The swelling kinetics of the developed hydrogel discs exhibited second-order kinetics. Moreover, the hydrogel discs responded to the concentration of electrolytes (CaCl2 and NaCl). The results of the FTIR confirm the formation of the hydrogel via free-radical polymerization. However, the major peaks of acyclovir remain intact, proving drug-excipient compatibility. The results of the SEM analysis reveal the porous, rough surface of the hydrogel discs with multiple cracks and pores over the surface. The results of the PXRD disclose the amorphous nature of the fabricated hydrogel. The dissolution studies showed a minor amount of acyclovir sodium released in an acidic environment, while an extended release up to 36 h in the phosphate buffer was observed. The drug release followed Hixen–Crowell’s kinetics with Fickian diffusion mechanism. The toxicity studies demonstrated the non-toxic nature of the polymeric carrier system. Therefore, these results signify the quince/mucin co-poly (methacrylate) hydrogel as a smart material with the potential to deliver acyclovir into the intestine for an extended period of time.
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