Preformulation of FK506 Prodrugs for Improving Solubility
DC Field | Value | Language |
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dc.contributor.author | Na, Young-Guk | - |
dc.contributor.author | Jun, Hye-Suk | - |
dc.contributor.author | Kim, Daehee | - |
dc.contributor.author | Park, Byong-Chul | - |
dc.contributor.author | Lim, Si-Kyu | - |
dc.contributor.author | Lee, Ki-Ho | - |
dc.contributor.author | Hwang, Sung-Joo | - |
dc.contributor.author | Park, Jeong-Sook | - |
dc.contributor.author | Jung, Sang-Hun | - |
dc.contributor.author | Cho, Cheong-Weon | - |
dc.date.accessioned | 2021-09-03T21:34:02Z | - |
dc.date.available | 2021-09-03T21:34:02Z | - |
dc.date.created | 2021-06-18 | - |
dc.date.issued | 2016-08 | - |
dc.identifier.issn | 0253-2964 | - |
dc.identifier.uri | https://scholar.korea.ac.kr/handle/2021.sw.korea/87975 | - |
dc.description.abstract | In order to improve water solubility of a lipophilic drug, tacrolimus (FK506), two prodrugs (FK506-G or FK506-S) such as FK506-M32-LS-G (FK506-G) and FK506-M32-LS-SL (FK506-S) were synthesized. Two prodrugs (FK506-G or FK506-S), including FK506, were characterized by differential scanning calorimetry (DSC), X-ray diffractometry (XRD), scanning electron microscopy (SEM), enzymatic kinetics, and cytotoxicity. A phase solubility test was conducted in distilled water, and the solubility of two prodrugs (FK506-G or FK506-S) was measured in various pH values for pH solubility profiles. Most interesting was that FK506-S showed the highest solubility, 866 g/mL in water. In vitro enzymatic kinetics of two prodrugs (FK506-G or FK506-S) in human plasma was evaluated by measuring the decrease of FK506-G or FK506-S as well as the increase of FK506 by HPLC, and FK506-G or FK506-S was metabolized in 1 h in human plasma. Two prodrugs (FK506-G or FK506-S) including FK506 showed an IC50 of 336.6 g/mL for FK506, 337.9 g/mL for FK506-G, or 480.1 g/mL for FK506-S against a conjunctive cell line, Clone 1-5c-4 cells. Taken together, FK506-S could be the most optimal prodrug for aqueous preparations based on preformulation data. | - |
dc.language | English | - |
dc.language.iso | en | - |
dc.publisher | WILEY-V C H VERLAG GMBH | - |
dc.subject | MESOPOROUS SILICA NANOPARTICLES | - |
dc.subject | CYTOTOXICITY | - |
dc.subject | FK-506 | - |
dc.subject | DOCETAXEL | - |
dc.subject | PHARMACOKINETICS | - |
dc.subject | STREPTOMYCES | - |
dc.subject | CYCLODEXTRIN | - |
dc.subject | DOXORUBICIN | - |
dc.subject | CURCUMIN | - |
dc.subject | INVITRO | - |
dc.title | Preformulation of FK506 Prodrugs for Improving Solubility | - |
dc.type | Article | - |
dc.contributor.affiliatedAuthor | Lee, Ki-Ho | - |
dc.identifier.doi | 10.1002/bkcs.10861 | - |
dc.identifier.scopusid | 2-s2.0-84979503401 | - |
dc.identifier.wosid | 000381037000024 | - |
dc.identifier.bibliographicCitation | BULLETIN OF THE KOREAN CHEMICAL SOCIETY, v.37, no.8, pp.1313 - 1319 | - |
dc.relation.isPartOf | BULLETIN OF THE KOREAN CHEMICAL SOCIETY | - |
dc.citation.title | BULLETIN OF THE KOREAN CHEMICAL SOCIETY | - |
dc.citation.volume | 37 | - |
dc.citation.number | 8 | - |
dc.citation.startPage | 1313 | - |
dc.citation.endPage | 1319 | - |
dc.type.rims | ART | - |
dc.type.docType | Article | - |
dc.identifier.kciid | ART002132093 | - |
dc.description.journalClass | 1 | - |
dc.description.journalRegisteredClass | scie | - |
dc.description.journalRegisteredClass | scopus | - |
dc.description.journalRegisteredClass | kci | - |
dc.relation.journalResearchArea | Chemistry | - |
dc.relation.journalWebOfScienceCategory | Chemistry, Multidisciplinary | - |
dc.subject.keywordPlus | MESOPOROUS SILICA NANOPARTICLES | - |
dc.subject.keywordPlus | CYTOTOXICITY | - |
dc.subject.keywordPlus | FK-506 | - |
dc.subject.keywordPlus | DOCETAXEL | - |
dc.subject.keywordPlus | PHARMACOKINETICS | - |
dc.subject.keywordPlus | STREPTOMYCES | - |
dc.subject.keywordPlus | CYCLODEXTRIN | - |
dc.subject.keywordPlus | DOXORUBICIN | - |
dc.subject.keywordPlus | CURCUMIN | - |
dc.subject.keywordPlus | INVITRO | - |
dc.subject.keywordAuthor | FK506 | - |
dc.subject.keywordAuthor | Prodrug | - |
dc.subject.keywordAuthor | Preformulation | - |
dc.subject.keywordAuthor | Cytotoxicity | - |
dc.subject.keywordAuthor | Solubility | - |
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