Preparation, Characterization, and <i>In Vitro</i> Evaluation of Chlorogenic Acid Loaded Hydrogel Beads for the Management of Ulcerative Colitis

<i>Ulcerative colitis (UC) is a chronic inflammatory colon disorder. Several modern medicines have been used for UC treatment but are associated with side effects. Hence, herbal medicine-inspired lead molecules are promising for managing UC. Chlorogenic acid (CGA), an herbal bioactive, has been reported for anti-inflammatory, anticancer, antioxidant, and immunomodulatory activity. The current study aimed to develop enteric-coated mucoadhesive beads of CGA for colon targeting. CGA-loaded beads were prepared using chitosan and carrageenan as polymers through an ionic gelation technique. Furthermore, beads were coated with Eudragit S-100. The formulations were characterized by particle size analyzer, ultraviolet (UV)-spectroscopy, Fourier transform infrared spectroscopy (FTIR), scanning electron microscope (SEM), and <i>in vitro</i> drug release study. The optimized formulation (CGA-F2) showed particle size (440.6 ± 6.1 μm), zeta potential (-31.12 ± 2.16 mV), entrapment efficiency (83.56 ± 5.46), %yield (86.87 ± 4.19), and drug loading (1.14 ± 0.09). SEM indicated that the morphologies of CGA-F2 were spherical and ellipsoidal. The FTIR study confirmed the compatibility of the drug with polymers used in the formulations. CGA-F2 exhibited mucoadhesive efficiency (94.33 ± 2.1%) and swelling index (0.98 ± 0.03) at simulated colonic fluid (SCF) pH 7.4 (<i>***p</i> < 0.001) significantly. In an <i>in vitro</i> drug release study, CGA-F2 (95.07 ± 3.85%) showed a sustained drug release profile in SCF (pH 7.4) at 37 ± 0.5°C for 24 h. Optimized formulation exhibited drug release in a sustained manner for 24 h, which may be due to the effect of mucoadhesive and enteric coating polymer. Hence, CGA-loaded beads would be promising for treating the UC.</i>

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Publication Details

Journal
Assay and Drug Development Technologies
Published
2024-12-04
DOI
https://doi.org/10.1089/adt.2024.072
Citations
2
Primary Topic
Inflammatory Bowel Disease
Type
article
Field-Weighted Citation Impact
1.10
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article

Preparation, Characterization, and In Vitro Evaluation of Chlorogenic Acid Loaded Hydrogel Beads for the Management of Ulcerative Colitis

Mohammad Akhlaquer Rahman, Ranjit K. Harwansh, Rohitas Deshmukh, Hemant Bhati
2 citations
Assay and Drug Development Technologies
Inflammatory Bowel Disease
1.10
article

Preparation, Characterization, and In Vitro Evaluation of Chlorogenic Acid Loaded Hydrogel Beads for the Management of Ulcerative Colitis

Mohammad Akhlaquer Rahman, Ranjit K. Harwansh, Rohitas Deshmukh, Hemant Bhati
article en
2 citations

Abstract

<i>Ulcerative colitis (UC) is a chronic inflammatory colon disorder. Several modern medicines have been used for UC treatment but are associated with side effects. Hence, herbal medicine-inspired lead molecules are promising for managing UC. Chlorogenic acid (CGA), an herbal bioactive, has been reported for anti-inflammatory, anticancer, antioxidant, and immunomodulatory activity. The current study aimed to develop enteric-coated mucoadhesive beads of CGA for colon targeting. CGA-loaded beads were prepared using chitosan and carrageenan as polymers through an ionic gelation technique. Furthermore, beads were coated with Eudragit S-100. The formulations were characterized by particle size analyzer, ultraviolet (UV)-spectroscopy, Fourier transform infrared spectroscopy (FTIR), scanning electron microscope (SEM), and <i>in vitro</i> drug release study. The optimized formulation (CGA-F2) showed particle size (440.6 ± 6.1 μm), zeta potential (-31.12 ± 2.16 mV), entrapment efficiency (83.56 ± 5.46), %yield (86.87 ± 4.19), and drug loading (1.14 ± 0.09). SEM indicated that the morphologies of CGA-F2 were spherical and ellipsoidal. The FTIR study confirmed the compatibility of the drug with polymers used in the formulations. CGA-F2 exhibited mucoadhesive efficiency (94.33 ± 2.1%) and swelling index (0.98 ± 0.03) at simulated colonic fluid (SCF) pH 7.4 (<i>***p</i> < 0.001) significantly. In an <i>in vitro</i> drug release study, CGA-F2 (95.07 ± 3.85%) showed a sustained drug release profile in SCF (pH 7.4) at 37 ± 0.5°C for 24 h. Optimized formulation exhibited drug release in a sustained manner for 24 h, which may be due to the effect of mucoadhesive and enteric coating polymer. Hence, CGA-loaded beads would be promising for treating the UC.</i>

Assay and Drug Development TechnologiesVol. 23(1)
Taif University (SA), GLA University (IN)
Zero hunger
Openalex Percentile: Top 18%
Inflammatory Bowel Disease
1.10
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