Fabrication of poly (butadiene-block-ethylene oxide) based amphiphilic polymersomes : an approach for improved oral pharmacokinetics of Sorafenib
Sorafenib (SFN), a hydrophobic anticancer drug, has several limitations predominantly poor aqueous solubility and hepatic first-pass effect, limiting its oral delivery that results into several other complications. Present study aims to develop Sorafenib loaded polymersomes using poly butadiene bloc...
| Main Authors: | , , , , , |
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| Format: | Journal Article |
| Language: | English |
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2020
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| Online Access: | https://hdl.handle.net/10356/141202 |
| _version_ | 1826122920326332416 |
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| author | Muhammad Adeeb Khan Shaukat Ali Venkatraman, Subbu S. Muhammad Farhan Sohail Muhammad Ovais Abida Raza |
| author2 | School of Materials Science and Engineering |
| author_facet | School of Materials Science and Engineering Muhammad Adeeb Khan Shaukat Ali Venkatraman, Subbu S. Muhammad Farhan Sohail Muhammad Ovais Abida Raza |
| author_sort | Muhammad Adeeb Khan |
| collection | NTU |
| description | Sorafenib (SFN), a hydrophobic anticancer drug, has several limitations predominantly poor aqueous solubility and hepatic first-pass effect, limiting its oral delivery that results into several other complications. Present study aims to develop Sorafenib loaded polymersomes using poly butadiene block poly ethylene oxide (PB-b-PEO), an amphiphilic co-block polymer. Prior to drug loading, critical aggregate concentration (CAC) of polymer was calculated for stable formulation synthesis. The developed SFN loaded PB-b-PEO polymersomes (SFN-PB-b-PEO, test formulation) characterized by DLS and cryo-TEM showed particle size 282 nm, polydispersity (PDI) of less than 0.29 and membrane thickness of about 20 nm. SFN-PB-b-PEO polymersomes demonstrated encapsulation efficiency of 71% and showed sustained drug release up to 144 h. Formulation remained stable for 3 months in suspension form. In vitro cytotoxicity against HepG2 cells showed 1.7 folds improved toxicity compared to SFN suspension. In addition, oral administration of SFN-PB-b-PEO polymersomes in BALB/c mice showed increased Cmax and AUC0-96 by 1.7 and 2.77-fold respectively (p < 0.05) compared to those of SFN suspension (reference formulation). Findings suggest that the SFN-PB-b-PEO polymersomes can be a potential candidate for oral delivery of SFN. |
| first_indexed | 2024-10-01T05:56:27Z |
| format | Journal Article |
| id | ntu-10356/141202 |
| institution | Nanyang Technological University |
| language | English |
| last_indexed | 2024-10-01T05:56:27Z |
| publishDate | 2020 |
| record_format | dspace |
| spelling | ntu-10356/1412022020-06-05T01:49:36Z Fabrication of poly (butadiene-block-ethylene oxide) based amphiphilic polymersomes : an approach for improved oral pharmacokinetics of Sorafenib Muhammad Adeeb Khan Shaukat Ali Venkatraman, Subbu S. Muhammad Farhan Sohail Muhammad Ovais Abida Raza School of Materials Science and Engineering Engineering::Materials Sorafenib Oral Delivery Sorafenib (SFN), a hydrophobic anticancer drug, has several limitations predominantly poor aqueous solubility and hepatic first-pass effect, limiting its oral delivery that results into several other complications. Present study aims to develop Sorafenib loaded polymersomes using poly butadiene block poly ethylene oxide (PB-b-PEO), an amphiphilic co-block polymer. Prior to drug loading, critical aggregate concentration (CAC) of polymer was calculated for stable formulation synthesis. The developed SFN loaded PB-b-PEO polymersomes (SFN-PB-b-PEO, test formulation) characterized by DLS and cryo-TEM showed particle size 282 nm, polydispersity (PDI) of less than 0.29 and membrane thickness of about 20 nm. SFN-PB-b-PEO polymersomes demonstrated encapsulation efficiency of 71% and showed sustained drug release up to 144 h. Formulation remained stable for 3 months in suspension form. In vitro cytotoxicity against HepG2 cells showed 1.7 folds improved toxicity compared to SFN suspension. In addition, oral administration of SFN-PB-b-PEO polymersomes in BALB/c mice showed increased Cmax and AUC0-96 by 1.7 and 2.77-fold respectively (p < 0.05) compared to those of SFN suspension (reference formulation). Findings suggest that the SFN-PB-b-PEO polymersomes can be a potential candidate for oral delivery of SFN. 2020-06-05T01:49:35Z 2020-06-05T01:49:35Z 2018 Journal Article Muhammad Adeeb Khan, Shaukat Ali, Venkatraman, S. S., Muhammad Farhan Sohail, Muhammad Ovais, Abida Raza. (2018). Fabrication of poly (butadiene-block-ethylene oxide) based amphiphilic polymersomes : an approach for improved oral pharmacokinetics of Sorafenib. International Journal of Pharmaceutics, 542(1-2), 196-204. doi:10.1016/j.ijpharm.2018.03.023 0378-5173 https://hdl.handle.net/10356/141202 10.1016/j.ijpharm.2018.03.023 29551745 2-s2.0-85043999420 1-2 542 196 204 en International Journal of Pharmaceutics © 2018 Elsevier B.V. All rights reserved. |
| spellingShingle | Engineering::Materials Sorafenib Oral Delivery Muhammad Adeeb Khan Shaukat Ali Venkatraman, Subbu S. Muhammad Farhan Sohail Muhammad Ovais Abida Raza Fabrication of poly (butadiene-block-ethylene oxide) based amphiphilic polymersomes : an approach for improved oral pharmacokinetics of Sorafenib |
| title | Fabrication of poly (butadiene-block-ethylene oxide) based amphiphilic polymersomes : an approach for improved oral pharmacokinetics of Sorafenib |
| title_full | Fabrication of poly (butadiene-block-ethylene oxide) based amphiphilic polymersomes : an approach for improved oral pharmacokinetics of Sorafenib |
| title_fullStr | Fabrication of poly (butadiene-block-ethylene oxide) based amphiphilic polymersomes : an approach for improved oral pharmacokinetics of Sorafenib |
| title_full_unstemmed | Fabrication of poly (butadiene-block-ethylene oxide) based amphiphilic polymersomes : an approach for improved oral pharmacokinetics of Sorafenib |
| title_short | Fabrication of poly (butadiene-block-ethylene oxide) based amphiphilic polymersomes : an approach for improved oral pharmacokinetics of Sorafenib |
| title_sort | fabrication of poly butadiene block ethylene oxide based amphiphilic polymersomes an approach for improved oral pharmacokinetics of sorafenib |
| topic | Engineering::Materials Sorafenib Oral Delivery |
| url | https://hdl.handle.net/10356/141202 |
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