Eudragit-Coated Sporopollenin Exine Microcapsules (SEMC) of <i>Phoenix dactylifera</i> L. of 5-Fluorouracil for Colon-Specific Drug Delivery
In this study, 5-fluorouracil (5-FU)-loaded pollens of Phoenix dactylifera and their coating with ERS was done and evaluated for the colon-targeted delivery of 5-FU to treat colon cancer. Sporopollenin exine microcapsules (SEMC) from the pollens of Phoenix dactylifera were extracted by the reflux me...
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| Format: | Article |
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MDPI AG
2021-11-01
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| Series: | Pharmaceutics |
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| Online Access: | https://www.mdpi.com/1999-4923/13/11/1921 |
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| author | Mohammad Raish Mohd Abul Kalam Ajaz Ahmad Mudassar Shahid Mushtaq Ahmad Ansari Abdul Ahad Raisuddin Ali Yousef A. Bin Jardan Aws Alshamsan Musaed Alkholief Khalid M. Alkharfy Ibrahim Abdelsalam Abdelrahman Fahad I. Al-Jenoobi |
| author_facet | Mohammad Raish Mohd Abul Kalam Ajaz Ahmad Mudassar Shahid Mushtaq Ahmad Ansari Abdul Ahad Raisuddin Ali Yousef A. Bin Jardan Aws Alshamsan Musaed Alkholief Khalid M. Alkharfy Ibrahim Abdelsalam Abdelrahman Fahad I. Al-Jenoobi |
| author_sort | Mohammad Raish |
| collection | DOAJ |
| description | In this study, 5-fluorouracil (5-FU)-loaded pollens of Phoenix dactylifera and their coating with ERS was done and evaluated for the colon-targeted delivery of 5-FU to treat colon cancer. Sporopollenin exine microcapsules (SEMC) from the pollens of Phoenix dactylifera were extracted by the reflux method and 5-FU into SEMC was encapsulated by the vacuum-assisted loading method. 5-FU loaded SEMC was coated with Eudragit<sup>®</sup> RS-100 (ERS) by the organic solvent-evaporation technique under vacuum to avoid the discharge of 5-FU in the stomach and small intestine. Morphological and physicochemical characterization of drug-loaded SEMC (coated/uncoated) was performed by scanning electron microscopy (SEM), FTIR, XRD, and DSC. The encapsulation and drug loading were determined by the direct method, and an in vitro release study was performed in simulated gastric and intestinal fluids (SGF/SIF). The colon-specific delivery of 5-FU from the SEMC was assessed in terms of pharmacokinetics and gastrointestinal tract distribution after oral administration in rats. The successful encapsulation and loading of 5-FU into SEMC by a vacuum-assisted loading technique and its coating with ERS by a solvent-evaporation technique were achieved. SEM images of uncoated SEMC have shown porous structures, and coating with ERS reserved their morphology with a smooth surface and discrete microstructures and the 5% <i>w/v</i> ERS acetone solution. ERS-coated SEMC sustained the release of 5-FU until 24 h in SIF, while it was up to 12 h only from uncoated SEMC. The maximum plasma concentration (Cmax) of 5-FU from uncoated SEMC was 102.82 μg/mL after 1 h, indicating a rapid release of 5-FU in the upper gastrointestinal tract. This concentration decreased quickly with a half-life of 4 h, AUC0-t was 264.1 μg/mL.h, and MRT0-inf was 5.2 h. The Cmax of 5-FU from ERS-coated SEMC was 19.47 μg/mL at 16 h. The Cmax of 5-FU in small intestines was 406.2 μg/g at 1 h from uncoated SEMC and 1271.5 μg/g at 12 h from coated SEMC. Conclusively, a 249.9-fold higher relative bioavailability of 5-FU was achieved with the ERS-coated SEMC in colon tissues than that from uncoated SEMC. |
| first_indexed | 2024-03-10T05:08:55Z |
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| id | doaj.art-5d365e09811a4bf393f5448c6fbf00cb |
| institution | Directory Open Access Journal |
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| language | English |
| last_indexed | 2024-03-10T05:08:55Z |
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| series | Pharmaceutics |
| spelling | doaj.art-5d365e09811a4bf393f5448c6fbf00cb2023-11-23T00:59:41ZengMDPI AGPharmaceutics1999-49232021-11-011311192110.3390/pharmaceutics13111921Eudragit-Coated Sporopollenin Exine Microcapsules (SEMC) of <i>Phoenix dactylifera</i> L. of 5-Fluorouracil for Colon-Specific Drug DeliveryMohammad Raish0Mohd Abul Kalam1Ajaz Ahmad2Mudassar Shahid3Mushtaq Ahmad Ansari4Abdul Ahad5Raisuddin Ali6Yousef A. Bin Jardan7Aws Alshamsan8Musaed Alkholief9Khalid M. Alkharfy10Ibrahim Abdelsalam Abdelrahman11Fahad I. Al-Jenoobi12Department of Pharmaceutics, College of Pharmacy, King Saud University, P.O. Box 2457, Riyadh 11451, Saudi ArabiaDepartment of Pharmaceutics, College of Pharmacy, King Saud University, P.O. Box 2457, Riyadh 11451, Saudi ArabiaDepartment of Clinical Pharmacy, College of Pharmacy, King Saud University, P.O. Box 2457, Riyadh 11451, Saudi ArabiaDepartment of Pharmaceutics, College of Pharmacy, King Saud University, P.O. Box 2457, Riyadh 11451, Saudi ArabiaDepartment of Pharmacology and Toxicology, College of Pharmacy, King Saud University, P.O. Box 2457, Riyadh 11451, Saudi ArabiaDepartment of Pharmaceutics, College of Pharmacy, King Saud University, P.O. Box 2457, Riyadh 11451, Saudi ArabiaDepartment of Pharmaceutics, College of Pharmacy, King Saud University, P.O. Box 2457, Riyadh 11451, Saudi ArabiaDepartment of Pharmaceutics, College of Pharmacy, King Saud University, P.O. Box 2457, Riyadh 11451, Saudi ArabiaDepartment of Pharmaceutics, College of Pharmacy, King Saud University, P.O. Box 2457, Riyadh 11451, Saudi ArabiaDepartment of Pharmaceutics, College of Pharmacy, King Saud University, P.O. Box 2457, Riyadh 11451, Saudi ArabiaDepartment of Clinical Pharmacy, College of Pharmacy, King Saud University, P.O. Box 2457, Riyadh 11451, Saudi ArabiaDepartment of Pharmaceutics, College of Pharmacy, King Saud University, P.O. Box 2457, Riyadh 11451, Saudi ArabiaDepartment of Pharmaceutics, College of Pharmacy, King Saud University, P.O. Box 2457, Riyadh 11451, Saudi ArabiaIn this study, 5-fluorouracil (5-FU)-loaded pollens of Phoenix dactylifera and their coating with ERS was done and evaluated for the colon-targeted delivery of 5-FU to treat colon cancer. Sporopollenin exine microcapsules (SEMC) from the pollens of Phoenix dactylifera were extracted by the reflux method and 5-FU into SEMC was encapsulated by the vacuum-assisted loading method. 5-FU loaded SEMC was coated with Eudragit<sup>®</sup> RS-100 (ERS) by the organic solvent-evaporation technique under vacuum to avoid the discharge of 5-FU in the stomach and small intestine. Morphological and physicochemical characterization of drug-loaded SEMC (coated/uncoated) was performed by scanning electron microscopy (SEM), FTIR, XRD, and DSC. The encapsulation and drug loading were determined by the direct method, and an in vitro release study was performed in simulated gastric and intestinal fluids (SGF/SIF). The colon-specific delivery of 5-FU from the SEMC was assessed in terms of pharmacokinetics and gastrointestinal tract distribution after oral administration in rats. The successful encapsulation and loading of 5-FU into SEMC by a vacuum-assisted loading technique and its coating with ERS by a solvent-evaporation technique were achieved. SEM images of uncoated SEMC have shown porous structures, and coating with ERS reserved their morphology with a smooth surface and discrete microstructures and the 5% <i>w/v</i> ERS acetone solution. ERS-coated SEMC sustained the release of 5-FU until 24 h in SIF, while it was up to 12 h only from uncoated SEMC. The maximum plasma concentration (Cmax) of 5-FU from uncoated SEMC was 102.82 μg/mL after 1 h, indicating a rapid release of 5-FU in the upper gastrointestinal tract. This concentration decreased quickly with a half-life of 4 h, AUC0-t was 264.1 μg/mL.h, and MRT0-inf was 5.2 h. The Cmax of 5-FU from ERS-coated SEMC was 19.47 μg/mL at 16 h. The Cmax of 5-FU in small intestines was 406.2 μg/g at 1 h from uncoated SEMC and 1271.5 μg/g at 12 h from coated SEMC. Conclusively, a 249.9-fold higher relative bioavailability of 5-FU was achieved with the ERS-coated SEMC in colon tissues than that from uncoated SEMC.https://www.mdpi.com/1999-4923/13/11/19215-fluorouracilpollen<i>Phoenix dactylifera</i>Eudragit<sup>®</sup>-RS100coatingcolon-specific |
| spellingShingle | Mohammad Raish Mohd Abul Kalam Ajaz Ahmad Mudassar Shahid Mushtaq Ahmad Ansari Abdul Ahad Raisuddin Ali Yousef A. Bin Jardan Aws Alshamsan Musaed Alkholief Khalid M. Alkharfy Ibrahim Abdelsalam Abdelrahman Fahad I. Al-Jenoobi Eudragit-Coated Sporopollenin Exine Microcapsules (SEMC) of <i>Phoenix dactylifera</i> L. of 5-Fluorouracil for Colon-Specific Drug Delivery Pharmaceutics 5-fluorouracil pollen <i>Phoenix dactylifera</i> Eudragit<sup>®</sup>-RS100 coating colon-specific |
| title | Eudragit-Coated Sporopollenin Exine Microcapsules (SEMC) of <i>Phoenix dactylifera</i> L. of 5-Fluorouracil for Colon-Specific Drug Delivery |
| title_full | Eudragit-Coated Sporopollenin Exine Microcapsules (SEMC) of <i>Phoenix dactylifera</i> L. of 5-Fluorouracil for Colon-Specific Drug Delivery |
| title_fullStr | Eudragit-Coated Sporopollenin Exine Microcapsules (SEMC) of <i>Phoenix dactylifera</i> L. of 5-Fluorouracil for Colon-Specific Drug Delivery |
| title_full_unstemmed | Eudragit-Coated Sporopollenin Exine Microcapsules (SEMC) of <i>Phoenix dactylifera</i> L. of 5-Fluorouracil for Colon-Specific Drug Delivery |
| title_short | Eudragit-Coated Sporopollenin Exine Microcapsules (SEMC) of <i>Phoenix dactylifera</i> L. of 5-Fluorouracil for Colon-Specific Drug Delivery |
| title_sort | eudragit coated sporopollenin exine microcapsules semc of i phoenix dactylifera i l of 5 fluorouracil for colon specific drug delivery |
| topic | 5-fluorouracil pollen <i>Phoenix dactylifera</i> Eudragit<sup>®</sup>-RS100 coating colon-specific |
| url | https://www.mdpi.com/1999-4923/13/11/1921 |
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