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...

Descripción completa

Guardado en:

Detalles Bibliográficos
Autores principales:	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
Formato:	article
Lenguaje:	EN
Publicado:	MDPI AG 2021
Materias:	5-fluorouracil pollen <i>Phoenix dactylifera</i> Eudragit<sup>®</sup>-RS100 coating colon-specific Pharmacy and materia medica RS1-441
Acceso en línea:	https://doaj.org/article/5d365e09811a4bf393f5448c6fbf00cb
Etiquetas:	Agregar Etiqueta Sin Etiquetas, Sea el primero en etiquetar este registro!

id	oai:doaj.org-article:5d365e09811a4bf393f5448c6fbf00cb
record_format	dspace
spelling	oai:doaj.org-article:5d365e09811a4bf393f5448c6fbf00cb2021-11-25T18:41:52ZEudragit-Coated Sporopollenin Exine Microcapsules (SEMC) of <i>Phoenix dactylifera</i> L. of 5-Fluorouracil for Colon-Specific Drug Delivery10.3390/pharmaceutics131119211999-4923https://doaj.org/article/5d365e09811a4bf393f5448c6fbf00cb2021-11-01T00:00:00Zhttps://www.mdpi.com/1999-4923/13/11/1921https://doaj.org/toc/1999-4923In 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.Mohammad RaishMohd Abul KalamAjaz AhmadMudassar ShahidMushtaq Ahmad AnsariAbdul AhadRaisuddin AliYousef A. Bin JardanAws AlshamsanMusaed AlkholiefKhalid M. AlkharfyIbrahim Abdelsalam AbdelrahmanFahad I. Al-JenoobiMDPI AGarticle5-fluorouracilpollen<i>Phoenix dactylifera</i>Eudragit<sup>®</sup>-RS100coatingcolon-specificPharmacy and materia medicaRS1-441ENPharmaceutics, Vol 13, Iss 1921, p 1921 (2021)
institution	DOAJ
collection	DOAJ
language	EN
topic	5-fluorouracil pollen <i>Phoenix dactylifera</i> Eudragit<sup>®</sup>-RS100 coating colon-specific Pharmacy and materia medica RS1-441
spellingShingle	5-fluorouracil pollen <i>Phoenix dactylifera</i> Eudragit<sup>®</sup>-RS100 coating colon-specific Pharmacy and materia medica RS1-441 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
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.
format	article
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
title	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_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_sort	eudragit-coated sporopollenin exine microcapsules (semc) of <i>phoenix dactylifera</i> l. of 5-fluorouracil for colon-specific drug delivery
publisher	MDPI AG
publishDate	2021
url	https://doaj.org/article/5d365e09811a4bf393f5448c6fbf00cb
work_keys_str_mv	AT mohammadraish eudragitcoatedsporopolleninexinemicrocapsulessemcofiphoenixdactyliferailof5fluorouracilforcolonspecificdrugdelivery AT mohdabulkalam eudragitcoatedsporopolleninexinemicrocapsulessemcofiphoenixdactyliferailof5fluorouracilforcolonspecificdrugdelivery AT ajazahmad eudragitcoatedsporopolleninexinemicrocapsulessemcofiphoenixdactyliferailof5fluorouracilforcolonspecificdrugdelivery AT mudassarshahid eudragitcoatedsporopolleninexinemicrocapsulessemcofiphoenixdactyliferailof5fluorouracilforcolonspecificdrugdelivery AT mushtaqahmadansari eudragitcoatedsporopolleninexinemicrocapsulessemcofiphoenixdactyliferailof5fluorouracilforcolonspecificdrugdelivery AT abdulahad eudragitcoatedsporopolleninexinemicrocapsulessemcofiphoenixdactyliferailof5fluorouracilforcolonspecificdrugdelivery AT raisuddinali eudragitcoatedsporopolleninexinemicrocapsulessemcofiphoenixdactyliferailof5fluorouracilforcolonspecificdrugdelivery AT yousefabinjardan eudragitcoatedsporopolleninexinemicrocapsulessemcofiphoenixdactyliferailof5fluorouracilforcolonspecificdrugdelivery AT awsalshamsan eudragitcoatedsporopolleninexinemicrocapsulessemcofiphoenixdactyliferailof5fluorouracilforcolonspecificdrugdelivery AT musaedalkholief eudragitcoatedsporopolleninexinemicrocapsulessemcofiphoenixdactyliferailof5fluorouracilforcolonspecificdrugdelivery AT khalidmalkharfy eudragitcoatedsporopolleninexinemicrocapsulessemcofiphoenixdactyliferailof5fluorouracilforcolonspecificdrugdelivery AT ibrahimabdelsalamabdelrahman eudragitcoatedsporopolleninexinemicrocapsulessemcofiphoenixdactyliferailof5fluorouracilforcolonspecificdrugdelivery AT fahadialjenoobi eudragitcoatedsporopolleninexinemicrocapsulessemcofiphoenixdactyliferailof5fluorouracilforcolonspecificdrugdelivery
_version_	1718410773767651328

Eudragit-Coated Sporopollenin Exine Microcapsules (SEMC) of <i>Phoenix dactylifera</i> L. of 5-Fluorouracil for Colon-Specific Drug Delivery

Ejemplares similares