Quality by design enabled formulation development of regorafenib monohydrate loaded PEGylated PLGA polymeric nanoparticles: Enhanced oral bioavailability and biopharmaceutical attributes
Objective(s): Using a quality-by-design methodology, the current research is aimed to prepare and enhance the PEGylated PLGA-loaded regorafenib monohydrate polymeric nanoparticles for enhancing oral bioavailability and biopharmaceutical attributes. The oral multi-kinase inhibitor inhibits VEGFR2-TIE...
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Mashhad University of Medical Sciences
2024-10-01
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| Series: | Nanomedicine Journal |
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| Online Access: | https://nmj.mums.ac.ir/article_24729_285ef57c987090066db90e2add2fc123.pdf |
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| author | Dhananjay Panigrahi Suryakanta Swain Pratap Sahu Debashish Ghose Bikash Ranjan Jena |
| author_facet | Dhananjay Panigrahi Suryakanta Swain Pratap Sahu Debashish Ghose Bikash Ranjan Jena |
| author_sort | Dhananjay Panigrahi |
| collection | DOAJ |
| description | Objective(s): Using a quality-by-design methodology, the current research is aimed to prepare and enhance the PEGylated PLGA-loaded regorafenib monohydrate polymeric nanoparticles for enhancing oral bioavailability and biopharmaceutical attributes. The oral multi-kinase inhibitor inhibits VEGFR2-TIE2 tyrosine kinases on two separate targets, which results in anti-angiogenic activity. It also inhibits stromal and oncogenic receptor tyrosine kinases. Materials and Methods: The current study developed nanosized, biocompatible, and PEGylated PLGA polymeric nanoparticles to administer regorafenib monohydrate to patients with metastatic colon cancer. This was accomplished using a modified nanoprecipitation technique to make drug-encapsulated PEGylated PLGA nanoparticles with poloxamer 188 as a stabilizer. Results: The polymeric nanoformulations were characterized for zeta potential, distribution of particle size, entrapment efficiency, DSC, FT-IR, X-RD, and SEM. Both in vitro and in vivo experimental studies were performed for the pure drug and the improved nanoparticle formulation.Conclusion: The nanoparticles obtained from optimization studies were found to have smaller particle sizes, higher entrapment efficiency (%), drug loading capacity, spherical shape particles, amorphous drug embedded matrix, and a biphasic delayed release pattern. These findings suggest that drug-loaded PEGylated PLGA nanoparticles are a potent formulation for the treatment of colon cancer, with improved oral bioavailability and biopharmaceutical properties. |
| format | Article |
| id | doaj-art-e3da27e1845b4146b887eaf224a841ef |
| institution | Kabale University |
| issn | 2322-3049 2322-5904 |
| language | English |
| publishDate | 2024-10-01 |
| publisher | Mashhad University of Medical Sciences |
| record_format | Article |
| series | Nanomedicine Journal |
| spelling | doaj-art-e3da27e1845b4146b887eaf224a841ef2025-08-20T03:31:51ZengMashhad University of Medical SciencesNanomedicine Journal2322-30492322-59042024-10-0111440141610.22038/nmj.2024.76842.186724729Quality by design enabled formulation development of regorafenib monohydrate loaded PEGylated PLGA polymeric nanoparticles: Enhanced oral bioavailability and biopharmaceutical attributesDhananjay Panigrahi0Suryakanta Swain1Pratap Sahu2Debashish Ghose3Bikash Ranjan Jena4School of Pharmaceutical Sciences (SPS), Siksha O Anusandhan Deemed to be University, Kalinga Nagar, Ghatikia, Bhubaneswar-751029, Odisha, IndiaAmity Institute of Pharmacy, Amity University, Major Arterial Road, AA II, Newtown, Kadampukur, Kolkata-700135, West Bengal, IndiaSchool of Pharmaceutical Sciences (SPS), Siksha O Anusandhan Deemed to be University, Kalinga Nagar, Ghatikia, Bhubaneswar-751029, Odisha, IndiaDepartment of Pharmaceutics, Roland Institute of Pharmaceutical Sciences, Berhampur-760010, Odisha, IndiaSchool of Pharmacy and Life Science, Centurion University of Technology and Management Bhubaneswar-751009, Odisha, IndiaObjective(s): Using a quality-by-design methodology, the current research is aimed to prepare and enhance the PEGylated PLGA-loaded regorafenib monohydrate polymeric nanoparticles for enhancing oral bioavailability and biopharmaceutical attributes. The oral multi-kinase inhibitor inhibits VEGFR2-TIE2 tyrosine kinases on two separate targets, which results in anti-angiogenic activity. It also inhibits stromal and oncogenic receptor tyrosine kinases. Materials and Methods: The current study developed nanosized, biocompatible, and PEGylated PLGA polymeric nanoparticles to administer regorafenib monohydrate to patients with metastatic colon cancer. This was accomplished using a modified nanoprecipitation technique to make drug-encapsulated PEGylated PLGA nanoparticles with poloxamer 188 as a stabilizer. Results: The polymeric nanoformulations were characterized for zeta potential, distribution of particle size, entrapment efficiency, DSC, FT-IR, X-RD, and SEM. Both in vitro and in vivo experimental studies were performed for the pure drug and the improved nanoparticle formulation.Conclusion: The nanoparticles obtained from optimization studies were found to have smaller particle sizes, higher entrapment efficiency (%), drug loading capacity, spherical shape particles, amorphous drug embedded matrix, and a biphasic delayed release pattern. These findings suggest that drug-loaded PEGylated PLGA nanoparticles are a potent formulation for the treatment of colon cancer, with improved oral bioavailability and biopharmaceutical properties.https://nmj.mums.ac.ir/article_24729_285ef57c987090066db90e2add2fc123.pdfbioavailability potentialpolymeric nanoparticlesquality by designregorafenib monohydratezeta potential |
| spellingShingle | Dhananjay Panigrahi Suryakanta Swain Pratap Sahu Debashish Ghose Bikash Ranjan Jena Quality by design enabled formulation development of regorafenib monohydrate loaded PEGylated PLGA polymeric nanoparticles: Enhanced oral bioavailability and biopharmaceutical attributes Nanomedicine Journal bioavailability potential polymeric nanoparticles quality by design regorafenib monohydrate zeta potential |
| title | Quality by design enabled formulation development of regorafenib monohydrate loaded PEGylated PLGA polymeric nanoparticles: Enhanced oral bioavailability and biopharmaceutical attributes |
| title_full | Quality by design enabled formulation development of regorafenib monohydrate loaded PEGylated PLGA polymeric nanoparticles: Enhanced oral bioavailability and biopharmaceutical attributes |
| title_fullStr | Quality by design enabled formulation development of regorafenib monohydrate loaded PEGylated PLGA polymeric nanoparticles: Enhanced oral bioavailability and biopharmaceutical attributes |
| title_full_unstemmed | Quality by design enabled formulation development of regorafenib monohydrate loaded PEGylated PLGA polymeric nanoparticles: Enhanced oral bioavailability and biopharmaceutical attributes |
| title_short | Quality by design enabled formulation development of regorafenib monohydrate loaded PEGylated PLGA polymeric nanoparticles: Enhanced oral bioavailability and biopharmaceutical attributes |
| title_sort | quality by design enabled formulation development of regorafenib monohydrate loaded pegylated plga polymeric nanoparticles enhanced oral bioavailability and biopharmaceutical attributes |
| topic | bioavailability potential polymeric nanoparticles quality by design regorafenib monohydrate zeta potential |
| url | https://nmj.mums.ac.ir/article_24729_285ef57c987090066db90e2add2fc123.pdf |
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