Optimization of solid self-dispersing micelle for enhancing dissolution and oral bioavailability of valsartan using Box-Behnken design
DC Field | Value | Language |
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dc.contributor.author | Goo Y.T. | - |
dc.contributor.author | Park S.Y. | - |
dc.contributor.author | Chae B.R. | - |
dc.contributor.author | Yoon H.Y. | - |
dc.contributor.author | Kim C.H. | - |
dc.contributor.author | Choi J.Y. | - |
dc.contributor.author | Song S.H. | - |
dc.contributor.author | Choi Y.W. | - |
dc.date.available | 2020-08-03T07:20:56Z | - |
dc.date.issued | 2020-07-30 | - |
dc.identifier.issn | 0378-5173 | - |
dc.identifier.issn | 1873-3476 | - |
dc.identifier.uri | https://scholarworks.bwise.kr/cau/handle/2019.sw.cau/42772 | - |
dc.description.abstract | A novel solid self-dispersing micelle (S-SDM) was developed to enhance the oral bioavailability of valsartan (VST) and to reduce the total mass of solidified supersaturable self-microemulsifying drug delivery system (S-SuSMEDDS), composed of Capmul MCM, Tween 80 (T80), Gelucire 44/14 (G44), Poloxamer 407, Florite PS-10 (FLO), and low-substituted hydroxypropyl cellulose B1 (HPC). Excluding oil component from S-SuSMEDDS, S-SDM was optimized using a Box-Behnken design with three independent variables: X1 (T80/G44, 0.63), X2 (FLO/HPC, 0.41), and X3 (solid carrier, 177.6 mg); and three response factors: Y1 (droplet size, 191.9 nm), Y2 (dissolution efficiency at 15 min, 55.0%), and Y3 (angle of repose, 32.4°). The desirability function was 0.636, showing an excellent agreement between the predicted and experimental values. With approximately 75% weight of S-SuSMEDDS, no distinct crystallinity of VST was observed in S-SDM, resulting in critical micelle concentration value of 32 μg/mL. Optimized S-SDM showed an approximate 4-fold improved dissolution (pH 1.2, 500 mL) compared with raw VST. Following oral administration in rats, optimized S-SDM improved relative bioavailability by approximately 235%, 216%, and 127% versus raw VST, Diovan® (commercial reference), and S-SuSMEDDS, respectively. Thus, optimized S-SDM could be a selectable candidate for developing water-insoluble drugs in reduced quantity. © 2020 Elsevier B.V. | - |
dc.format.extent | 11 | - |
dc.language | 영어 | - |
dc.language.iso | ENG | - |
dc.publisher | Elsevier B.V. | - |
dc.title | Optimization of solid self-dispersing micelle for enhancing dissolution and oral bioavailability of valsartan using Box-Behnken design | - |
dc.type | Article | - |
dc.identifier.doi | 10.1016/j.ijpharm.2020.119483 | - |
dc.identifier.bibliographicCitation | International Journal of Pharmaceutics, v.585, pp 1 - 11 | - |
dc.description.isOpenAccess | N | - |
dc.identifier.wosid | 000549823500011 | - |
dc.identifier.scopusid | 2-s2.0-85086652046 | - |
dc.citation.endPage | 11 | - |
dc.citation.startPage | 1 | - |
dc.citation.title | International Journal of Pharmaceutics | - |
dc.citation.volume | 585 | - |
dc.type.docType | Article | - |
dc.publisher.location | 네델란드 | - |
dc.subject.keywordAuthor | Box-Behnken design | - |
dc.subject.keywordAuthor | Dissolution | - |
dc.subject.keywordAuthor | Oral bioavailability | - |
dc.subject.keywordAuthor | Reduced quantity | - |
dc.subject.keywordAuthor | Solid self-dispersing micelle | - |
dc.subject.keywordAuthor | Valsartan | - |
dc.subject.keywordPlus | DRUG-DELIVERY-SYSTEM | - |
dc.subject.keywordPlus | INTESTINAL PERMEABILITY | - |
dc.subject.keywordPlus | ATORVASTATIN CALCIUM | - |
dc.subject.keywordPlus | ABSORPTION | - |
dc.subject.keywordPlus | SMEDDS | - |
dc.subject.keywordPlus | TOOL | - |
dc.subject.keywordPlus | SOLIDIFICATION | - |
dc.subject.keywordPlus | FLUORESCENCE | - |
dc.subject.keywordPlus | SPECTROSCOPY | - |
dc.subject.keywordPlus | ENHANCEMENT | - |
dc.relation.journalResearchArea | Pharmacology & Pharmacy | - |
dc.relation.journalWebOfScienceCategory | Pharmacology & Pharmacy | - |
dc.description.journalRegisteredClass | scie | - |
dc.description.journalRegisteredClass | scopus | - |
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