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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| Main Authors: | , , , , |
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| Format: | Article |
| Language: | English |
| Published: |
Mashhad University of Medical Sciences
2024-10-01
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| Series: | Nanomedicine Journal |
| Subjects: | |
| Online Access: | https://nmj.mums.ac.ir/article_24729_285ef57c987090066db90e2add2fc123.pdf |
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| Summary: | 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. |
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| ISSN: | 2322-3049 2322-5904 |