Abstract
In designing an effective oral delivery system, the harshness of the gastrointestinal tract is a key limitation. Therefore, developing a pH-responsive carrier is crucial. We designed a chitosan/fucoidan nanoparticle (CS/F NP) and evaluated its potential as an oral delivery carrier. The results indicate that the CS/F NPs were successfully prepared based on their electrostatic interactions. They were approximately 380 nm, revealing significant pH-sensitive properties as the weight ratio of CS to F was 1:1. The isoelectric point of the CS/F NPs was 5.7. Using gamma scintigraphy, the 99m Tc-methylene diphosphonate encapsulated CS/F NPs were quite stable at pH 2.5 and decomposed at pH 7.4. For long-term storage, trehalose (20 %, w/v) is a suitable cryoprotectant. The outcome of the transepithelial electric resistance (TEER) of the Caco-2 monolayer shows that CS/F NPs effectively enhanced the opening of the cell tight junction. Briefly, the CS/F NPs developed are promising carriers for an oral delivery system.
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Acknowledgments
The authors would like to thank the National Science Council of Taiwan for financially supporting this research under Contract No. NSC 102-2221-E-019-004 and NSC 101-2113-M-400-001-MY2. The authors are also grateful to the National Nanoscience and Nanotechnology Program for the Innovative Molecular Biomedical Nano-Imaging Open Facility, the National Health Research Institutes (NM-101-PP-11), and the Animal Molecular Imaging Core Facility at NHRI (NM-101-PP-04) for performing radio-labeling and gamma scintigraphy for 99mTc-CS/F NPs. We also thank Miss Su-Chin Huang, Chin-Ya Chen, and Nai-Chun Huang for analytical supports of gel electrophoresis and size exclusion chromatography.
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Huang, YC., Chen, JK., Lam, UI. et al. Preparing, characterizing, and evaluating chitosan/fucoidan nanoparticles as oral delivery carriers. J Polym Res 21, 415 (2014). https://doi.org/10.1007/s10965-014-0415-6
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DOI: https://doi.org/10.1007/s10965-014-0415-6