Development of Novel pH-Sensitive Eudragit Coated Beads Containing Curcumin-Mesalamine Combination for Colon-Specific Drug Delivery
This research aims to develop a drug delivery system that effectively treats colitis while administering curcumin/mesalamine by coating alginate/chitosan beads with Eudragit® S-100 to target the colon. Beads were tested to determine their physicochemical characteristics. Coating with Eudragit® S-100...
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| Language: | English |
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MDPI AG
2023-03-01
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| Online Access: | https://www.mdpi.com/2310-2861/9/4/264 |
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| author | Eman J. Heikal Rashad M. Kaoud Shadeed Gad Hatem I. Mokhtar Abdullah Alattar Reem Alshaman Sawsan A. Zaitone Yasser M. Moustafa Taha M. Hammady |
| author_facet | Eman J. Heikal Rashad M. Kaoud Shadeed Gad Hatem I. Mokhtar Abdullah Alattar Reem Alshaman Sawsan A. Zaitone Yasser M. Moustafa Taha M. Hammady |
| author_sort | Eman J. Heikal |
| collection | DOAJ |
| description | This research aims to develop a drug delivery system that effectively treats colitis while administering curcumin/mesalamine by coating alginate/chitosan beads with Eudragit® S-100 to target the colon. Beads were tested to determine their physicochemical characteristics. Coating with Eudragit® S-100 prevents drug release at a pH of less than 7; this was demonstrated by in-vitro release conducted in a medium with gradually varying pH to mimic circumstances in various regions of the gastrointestinal tract. This study examined the efficacy of the coated beads in treating acetic acid-induced colitis in rats. Results showed that spherical beads were formed with an average diameter of 1.6–2.8 mm, and the obtained swelling ranged from 409.80% to 890.19%. The calculated entrapment efficiency ranged from 87.49% to 97.89%. The optimized formula F13 (which was composed of mesalamine-curcumin active ingredients, Sodium alginate as a gelling agent, chitosan as a controlled release agent, CaCl2 as a crosslinking agent, and Eudragit S-100 as a pH-sensitive coating agent) demonstrated the best entrapment efficiency (97.89% ± 1.66), swelling (890.19% ± 60.1), and bead size (2.7 ± 0.62 mm). In formulation #13, which was coated with Eudragit S 100, curcumin (6.01 ± 0.04%) and mesalamine (8.64 ± 0.7%), were released after 2 h at pH 1.2; 6.36 ± 0.11% and 10.45 ± 1.52% of curcumin and mesalamine, respectively, were then released after 4 h and at pH 6.8. Meanwhile, at pH 7.4, after 24 h, approximately 85.34 ± 2.3% (curcumin) and 91.5 ± 1.2% (mesalamine) were released. Formula #13 significantly reduced the colitis, and this suggests that the developed hydrogel beads can be used for delivering curcumin-mesalamine combinations to treat ulcerative colitis after adequate research. |
| first_indexed | 2024-03-11T05:00:35Z |
| format | Article |
| id | doaj.art-e462dc0e1d7f4582b594099b8cef9525 |
| institution | Directory Open Access Journal |
| issn | 2310-2861 |
| language | English |
| last_indexed | 2024-03-11T05:00:35Z |
| publishDate | 2023-03-01 |
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| record_format | Article |
| series | Gels |
| spelling | doaj.art-e462dc0e1d7f4582b594099b8cef95252023-11-17T19:20:59ZengMDPI AGGels2310-28612023-03-019426410.3390/gels9040264Development of Novel pH-Sensitive Eudragit Coated Beads Containing Curcumin-Mesalamine Combination for Colon-Specific Drug DeliveryEman J. Heikal0Rashad M. Kaoud1Shadeed Gad2Hatem I. Mokhtar3Abdullah Alattar4Reem Alshaman5Sawsan A. Zaitone6Yasser M. Moustafa7Taha M. Hammady8Department of Pharmaceutics and Industrial Pharmacy, Faculty of Pharmacy, Suez Canal University, Ismailia 41522, EgyptPharmacy Department, Ashur University College, Baghdad 10047, IraqDepartment of Pharmaceutics and Industrial Pharmacy, Faculty of Pharmacy, Suez Canal University, Ismailia 41522, EgyptDepartment of Pharmaceutical Chemistry, Faculty of Pharmacy, Sinai University-Kantara Branch, Ismailia 41636, EgyptDepartment of Pharmacology & Toxicology, Faculty of Pharmacy, University of Tabuk, Tabuk 71491, Saudi ArabiaDepartment of Pharmacology & Toxicology, Faculty of Pharmacy, University of Tabuk, Tabuk 71491, Saudi ArabiaDepartment of Pharmacology & Toxicology, Faculty of Pharmacy, University of Tabuk, Tabuk 71491, Saudi ArabiaDepartment of Pharmacology and Toxicology, Faculty of Pharmacy, Suez Canal University, Ismailia 41522, EgyptDepartment of Pharmaceutics and Industrial Pharmacy, Faculty of Pharmacy, Suez Canal University, Ismailia 41522, EgyptThis research aims to develop a drug delivery system that effectively treats colitis while administering curcumin/mesalamine by coating alginate/chitosan beads with Eudragit® S-100 to target the colon. Beads were tested to determine their physicochemical characteristics. Coating with Eudragit® S-100 prevents drug release at a pH of less than 7; this was demonstrated by in-vitro release conducted in a medium with gradually varying pH to mimic circumstances in various regions of the gastrointestinal tract. This study examined the efficacy of the coated beads in treating acetic acid-induced colitis in rats. Results showed that spherical beads were formed with an average diameter of 1.6–2.8 mm, and the obtained swelling ranged from 409.80% to 890.19%. The calculated entrapment efficiency ranged from 87.49% to 97.89%. The optimized formula F13 (which was composed of mesalamine-curcumin active ingredients, Sodium alginate as a gelling agent, chitosan as a controlled release agent, CaCl2 as a crosslinking agent, and Eudragit S-100 as a pH-sensitive coating agent) demonstrated the best entrapment efficiency (97.89% ± 1.66), swelling (890.19% ± 60.1), and bead size (2.7 ± 0.62 mm). In formulation #13, which was coated with Eudragit S 100, curcumin (6.01 ± 0.04%) and mesalamine (8.64 ± 0.7%), were released after 2 h at pH 1.2; 6.36 ± 0.11% and 10.45 ± 1.52% of curcumin and mesalamine, respectively, were then released after 4 h and at pH 6.8. Meanwhile, at pH 7.4, after 24 h, approximately 85.34 ± 2.3% (curcumin) and 91.5 ± 1.2% (mesalamine) were released. Formula #13 significantly reduced the colitis, and this suggests that the developed hydrogel beads can be used for delivering curcumin-mesalamine combinations to treat ulcerative colitis after adequate research.https://www.mdpi.com/2310-2861/9/4/264curcumincolon-specific deliveryhydrogel beadsmesalamineratulcerative colitis |
| spellingShingle | Eman J. Heikal Rashad M. Kaoud Shadeed Gad Hatem I. Mokhtar Abdullah Alattar Reem Alshaman Sawsan A. Zaitone Yasser M. Moustafa Taha M. Hammady Development of Novel pH-Sensitive Eudragit Coated Beads Containing Curcumin-Mesalamine Combination for Colon-Specific Drug Delivery Gels curcumin colon-specific delivery hydrogel beads mesalamine rat ulcerative colitis |
| title | Development of Novel pH-Sensitive Eudragit Coated Beads Containing Curcumin-Mesalamine Combination for Colon-Specific Drug Delivery |
| title_full | Development of Novel pH-Sensitive Eudragit Coated Beads Containing Curcumin-Mesalamine Combination for Colon-Specific Drug Delivery |
| title_fullStr | Development of Novel pH-Sensitive Eudragit Coated Beads Containing Curcumin-Mesalamine Combination for Colon-Specific Drug Delivery |
| title_full_unstemmed | Development of Novel pH-Sensitive Eudragit Coated Beads Containing Curcumin-Mesalamine Combination for Colon-Specific Drug Delivery |
| title_short | Development of Novel pH-Sensitive Eudragit Coated Beads Containing Curcumin-Mesalamine Combination for Colon-Specific Drug Delivery |
| title_sort | development of novel ph sensitive eudragit coated beads containing curcumin mesalamine combination for colon specific drug delivery |
| topic | curcumin colon-specific delivery hydrogel beads mesalamine rat ulcerative colitis |
| url | https://www.mdpi.com/2310-2861/9/4/264 |
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