Optimization of phytic acid-crosslinked chitosan microspheres for oral insulin delivery using response surface methodology
DC Field | Value | Language |
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dc.contributor.author | JEONG UN KIM | - |
dc.contributor.author | Hafiz Muhammad Shahbaz | - |
dc.contributor.author | Hyunah Lee | - |
dc.contributor.author | KIM TAEHYUNG | - |
dc.contributor.author | KYUNGJIK YANG | - |
dc.contributor.author | Young Hoon Roh | - |
dc.contributor.author | Jiyong Park | - |
dc.date.accessioned | 2021-12-01T02:40:17Z | - |
dc.date.available | 2021-12-01T02:40:17Z | - |
dc.date.issued | 2020-10 | - |
dc.identifier.issn | 0378-5173 | - |
dc.identifier.uri | https://yscholarhub.yonsei.ac.kr/handle/2021.sw.yonsei/5306 | - |
dc.description.abstract | Although oral administration is favorable mode of insulin delivery, it is the most challenging route, owing to poor oral bioavailability. In this study, a chitosan (CS)-based insulin delivery system was developed by ionic crosslinking with phytic acid (PA). CS-PA microspheres were optimized with different crosslinking conditions of CS and PA using response surface methodology to retain insulin during preparation and gastric digestion. Furthermore, the in vitro release profile, morphological structure, cytotoxicity, and intestinal permeability of the optimized microspheres, and its hypoglycemic effect in diabetic rats were evaluated. Under optimal conditions, the entrapment efficiency was 97.1%, and 67.0% of insulin was retained in the microspheres after 2 h of gastric digestion followed by a sustained-release in intestinal fluid. Insulin was primarily distributed in the microsphere core with a monodisperse diameter of 663.3 μm. The microspheres increased the permeability of insulin across Caco-2/HT-29 monolayers by 1.6 times with negligible cytotoxicity. The microspheres had a relative pharmacological bioavailability of 10.6% and significantly reduced blood glucose levels with a long-lasting hypoglycemic effect after oral administration in diabetic rats. This study demonstrated that an optimized formulation of a simple ionic crosslinking system using CS and PA could facilitate efficient oral delivery of insulin. | - |
dc.language | 영어 | - |
dc.language.iso | ENG | - |
dc.publisher | ELSEVIER SCIENCE BV | - |
dc.title | Optimization of phytic acid-crosslinked chitosan microspheres for oral insulin delivery using response surface methodology | - |
dc.type | Article | - |
dc.publisher.location | 네델란드 | - |
dc.identifier.doi | 10.1016/j.ijpharm.2020.119736 | - |
dc.identifier.scopusid | 2-s2.0-85089484758 | - |
dc.identifier.wosid | 000577558100014 | - |
dc.identifier.bibliographicCitation | INTERNATIONAL JOURNAL OF PHARMACEUTICS, v.588, pp 119736-1 - 119736-10 | - |
dc.citation.title | INTERNATIONAL JOURNAL OF PHARMACEUTICS | - |
dc.citation.volume | 588 | - |
dc.citation.startPage | 119736-1 | - |
dc.citation.endPage | 119736-10 | - |
dc.description.isOpenAccess | N | - |
dc.description.journalRegisteredClass | scie | - |
dc.description.journalRegisteredClass | scopus | - |
dc.subject.keywordPlus | chitosan nanoparticle | - |
dc.subject.keywordPlus | glucose | - |
dc.subject.keywordPlus | microsphere | - |
dc.subject.keywordPlus | phytic acid | - |
dc.subject.keywordPlus | recombinant human insulin | - |
dc.subject.keywordPlus | animal cell | - |
dc.subject.keywordPlus | animal experiment | - |
dc.subject.keywordPlus | animal model | - |
dc.subject.keywordPlus | animal tissue | - |
dc.subject.keywordPlus | antidiabetic activity | - |
dc.subject.keywordPlus | Article | - |
dc.subject.keywordPlus | Caco-2 cell line | - |
dc.subject.keywordPlus | chemical structure | - |
dc.subject.keywordPlus | circular dichroism | - |
dc.subject.keywordPlus | comparative study | - |
dc.subject.keywordPlus | controlled study | - |
dc.subject.keywordPlus | cross linking | - |
dc.subject.keywordPlus | cytotoxicity | - |
dc.subject.keywordPlus | digestion | - |
dc.subject.keywordPlus | drug bioavailability | - |
dc.subject.keywordPlus | drug delivery system | - |
dc.subject.keywordPlus | drug formulation | - |
dc.subject.keywordPlus | drug megadose | - |
dc.subject.keywordPlus | enzymatic degradation | - |
dc.subject.keywordPlus | glucose blood level | - |
dc.subject.keywordPlus | HT-29 cell line | - |
dc.subject.keywordPlus | in vitro study | - |
dc.subject.keywordPlus | insulin treatment | - |
dc.subject.keywordPlus | intestine fluid | - |
dc.subject.keywordPlus | intestine mucosa permeability | - |
dc.subject.keywordPlus | low drug dose | - |
dc.subject.keywordPlus | male | - |
dc.subject.keywordPlus | nanopharmaceutics | - |
dc.subject.keywordPlus | nonhuman | - |
dc.subject.keywordPlus | particle size | - |
dc.subject.keywordPlus | priority journal | - |
dc.subject.keywordPlus | process optimization | - |
dc.subject.keywordPlus | rat | - |
dc.subject.keywordPlus | response surface method | - |
dc.subject.keywordPlus | stomach juice | - |
dc.subject.keywordPlus | streptozotocin-induced diabetes mellitus | - |
dc.subject.keywordPlus | sustained drug release | - |
dc.subject.keywordAuthor | Oral insulin delivery | - |
dc.subject.keywordAuthor | Chitosan | - |
dc.subject.keywordAuthor | Phytic acid | - |
dc.subject.keywordAuthor | Ionic crosslinking | - |
dc.subject.keywordAuthor | Response surface methodology | - |
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