A novel 5-Fluorocuracil multiple-nanoemulsion used for the enhancement of oral bioavailability in the treatment of colorectal cancer
5-Fluorouracil (5-FU) is a drug of choice for colorectal-cancer. But oral therapeutic efficacy of 5-FU is restricted due to their very little bioavailability because of poor membrane permeability and GIT-absorption. We have developed a multiple nanoemulsion (w/o/w i.e. 5-FU-MNE) in which 5-FU incorp...
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| Format: | Article |
| Language: | English |
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Elsevier
2022-05-01
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| Series: | Saudi Journal of Biological Sciences |
| Subjects: | |
| Online Access: | http://www.sciencedirect.com/science/article/pii/S1319562X22000936 |
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| author | Niyaz Ahmad Ahmed A. Albassam Mohd Faiyaz Khan Zabih Ullah Taysser Mohammed Buheazah Hussain Salman AlHomoud Hassan Ali Al-Nasif |
| author_facet | Niyaz Ahmad Ahmed A. Albassam Mohd Faiyaz Khan Zabih Ullah Taysser Mohammed Buheazah Hussain Salman AlHomoud Hassan Ali Al-Nasif |
| author_sort | Niyaz Ahmad |
| collection | DOAJ |
| description | 5-Fluorouracil (5-FU) is a drug of choice for colorectal-cancer. But oral therapeutic efficacy of 5-FU is restricted due to their very little bioavailability because of poor membrane permeability and GIT-absorption. We have developed a multiple nanoemulsion (w/o/w i.e. 5-FU-MNE) in which 5-FU incorporated to improve their oral-absorption. Globule-size of opt-5-FU-MNE was 51.64 ± 2.61 nm with PDI and ZP 0.101 ± 0.001 and −5.59 ± 0.94, respectively. In vitro 5-FU-release and ex vivo permeation studies exhibited 99.71% release and 83.64% of 5-FU from opt-nanoformulation. Cytotoxic in vitro studies-exhibited that 5-FU in opt-5-FU-MNE was 5-times more potent than 5-FU-S on human-colon-cancer-cell-lines (HT-29). The enhanced Cmax with AUC0-8h with opt-5-FU-MNE was shown extremely significant (p < 0.001) in wistar rat’s plasma in the comparison of oral and i.v. treated group of 5-FU-S by PK-observations. Furthermore, opt-5-FU-MNE was showed much more significant (p < 0.001) results as compared to 5-FU-S (free) on cell lines for human colon cancer (HT-29). |
| first_indexed | 2024-04-11T17:35:04Z |
| format | Article |
| id | doaj.art-e71efb5e233d48a9ab476af1b3ab83ac |
| institution | Directory Open Access Journal |
| issn | 1319-562X |
| language | English |
| last_indexed | 2024-04-11T17:35:04Z |
| publishDate | 2022-05-01 |
| publisher | Elsevier |
| record_format | Article |
| series | Saudi Journal of Biological Sciences |
| spelling | doaj.art-e71efb5e233d48a9ab476af1b3ab83ac2022-12-22T04:11:39ZengElsevierSaudi Journal of Biological Sciences1319-562X2022-05-0129537043716A novel 5-Fluorocuracil multiple-nanoemulsion used for the enhancement of oral bioavailability in the treatment of colorectal cancerNiyaz Ahmad0Ahmed A. Albassam1Mohd Faiyaz Khan2Zabih Ullah3Taysser Mohammed Buheazah4Hussain Salman AlHomoud5Hassan Ali Al-Nasif6Department of Pharmaceutics, College of Clinical Pharmacy, Imam Abdulrahman Bin Faisal University, Dammam, Saudi Arabia; Corresponding author at: Department of Pharmaceutics, College of Clinical Pharmacy, Imam Abdulrahman Bin Faisal University, P.O. Box 1982, Dammam 31441, Saudi Arabia.Department of Clinical Pharmacy, College of Pharmacy, Prince Sattam bin Abdulaziz University, Alkharj, Saudi ArabiaDepartment of Clinical Pharmacy, College of Pharmacy, Prince Sattam bin Abdulaziz University, Alkharj, Saudi ArabiaDepartment of Pharmaceutical Sciences, College of Pharmacy and Dentistry, Buraydah Colleges, Alqassim, Saudi ArabiaDepartment of Pharmaceutics, College of Clinical Pharmacy, Imam Abdulrahman Bin Faisal University, Dammam, Saudi ArabiaDepartment of Pharmaceutics, College of Clinical Pharmacy, Imam Abdulrahman Bin Faisal University, Dammam, Saudi ArabiaDepartment of Pharmaceutics, College of Clinical Pharmacy, Imam Abdulrahman Bin Faisal University, Dammam, Saudi Arabia5-Fluorouracil (5-FU) is a drug of choice for colorectal-cancer. But oral therapeutic efficacy of 5-FU is restricted due to their very little bioavailability because of poor membrane permeability and GIT-absorption. We have developed a multiple nanoemulsion (w/o/w i.e. 5-FU-MNE) in which 5-FU incorporated to improve their oral-absorption. Globule-size of opt-5-FU-MNE was 51.64 ± 2.61 nm with PDI and ZP 0.101 ± 0.001 and −5.59 ± 0.94, respectively. In vitro 5-FU-release and ex vivo permeation studies exhibited 99.71% release and 83.64% of 5-FU from opt-nanoformulation. Cytotoxic in vitro studies-exhibited that 5-FU in opt-5-FU-MNE was 5-times more potent than 5-FU-S on human-colon-cancer-cell-lines (HT-29). The enhanced Cmax with AUC0-8h with opt-5-FU-MNE was shown extremely significant (p < 0.001) in wistar rat’s plasma in the comparison of oral and i.v. treated group of 5-FU-S by PK-observations. Furthermore, opt-5-FU-MNE was showed much more significant (p < 0.001) results as compared to 5-FU-S (free) on cell lines for human colon cancer (HT-29).http://www.sciencedirect.com/science/article/pii/S1319562X220009365-FluorouracilMultiple-nanoemulsion (w/o/w)Enhancement of oral bioavailabilityUHPLC-MS/MS bioanalytical-methodPharmacokineticsChemoprevention of colorectal cancer |
| spellingShingle | Niyaz Ahmad Ahmed A. Albassam Mohd Faiyaz Khan Zabih Ullah Taysser Mohammed Buheazah Hussain Salman AlHomoud Hassan Ali Al-Nasif A novel 5-Fluorocuracil multiple-nanoemulsion used for the enhancement of oral bioavailability in the treatment of colorectal cancer Saudi Journal of Biological Sciences 5-Fluorouracil Multiple-nanoemulsion (w/o/w) Enhancement of oral bioavailability UHPLC-MS/MS bioanalytical-method Pharmacokinetics Chemoprevention of colorectal cancer |
| title | A novel 5-Fluorocuracil multiple-nanoemulsion used for the enhancement of oral bioavailability in the treatment of colorectal cancer |
| title_full | A novel 5-Fluorocuracil multiple-nanoemulsion used for the enhancement of oral bioavailability in the treatment of colorectal cancer |
| title_fullStr | A novel 5-Fluorocuracil multiple-nanoemulsion used for the enhancement of oral bioavailability in the treatment of colorectal cancer |
| title_full_unstemmed | A novel 5-Fluorocuracil multiple-nanoemulsion used for the enhancement of oral bioavailability in the treatment of colorectal cancer |
| title_short | A novel 5-Fluorocuracil multiple-nanoemulsion used for the enhancement of oral bioavailability in the treatment of colorectal cancer |
| title_sort | novel 5 fluorocuracil multiple nanoemulsion used for the enhancement of oral bioavailability in the treatment of colorectal cancer |
| topic | 5-Fluorouracil Multiple-nanoemulsion (w/o/w) Enhancement of oral bioavailability UHPLC-MS/MS bioanalytical-method Pharmacokinetics Chemoprevention of colorectal cancer |
| url | http://www.sciencedirect.com/science/article/pii/S1319562X22000936 |
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