Cited 19 times in
Nanoparticulation improves bioavailability of Erlotinib
DC Field | Value | Language |
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dc.contributor.author | 김건홍 | - |
dc.contributor.author | 양경미 | - |
dc.date.accessioned | 2018-07-20T08:34:14Z | - |
dc.date.available | 2018-07-20T08:34:14Z | - |
dc.date.issued | 2017 | - |
dc.identifier.issn | 0363-9045 | - |
dc.identifier.uri | https://ir.ymlib.yonsei.ac.kr/handle/22282913/161293 | - |
dc.description.abstract | OBJECTIVES: Nanoparticulation using fat and supercritical fluid (NUFSTM) is a drug delivery platform technology enabling efficient and effective formulation of poorly soluble drugs. We performed experiments to examine whether NUFS™ could improve poor bioavailability and reduce fed-fasted bioavailability variances of erlotinib (Ert). METHODS: NUFS-Ert was prepared using NUFS™ technology; its physical properties were characterized, and drug release was measured. Furthermore, in vitro and in vivo efficacy tests and pharmacokinetic analysis were performed. RESULTS: NUFS-Ert nanoparticles had an average size of 250 nm and were stable for 2 months at 40 °C, 4 °C, and room temperature. The dissolution rate of NUFS-Ert increased in bio-relevant dissolution media. NUFS-Ert was more potent in inhibiting EGF signaling and in suppressing the proliferation of A549, a human non-small cell lung cancer cell line. Furthermore, A549 xenografts in BALB/c nude mice treated with NUFS-Ert regressed more efficiently than those in the mice treated with vehicle or Tarceva®. In addition, experimental lung metastasis was more efficiently inhibited by NUFS-Ert than by Tarceva®. The relative bioavailability of NUFS-Ert compared with that of Tarceva® was 550% and the ratio of the area under the concentration-time curve (AUC) of fed state to the AUC of fasted state was 1.8 for NUFS-Ert and 5.8 for Tarceva®. CONCLUSIONS: NUFS-Ert could improve poor bioavailability and reduce fed-fasted bioavailability variances of Ert. NUFS-Ert was more efficacious than Tarceva®. | - |
dc.description.statementOfResponsibility | restriction | - |
dc.language | England | - |
dc.publisher | 1520-5762 | - |
dc.relation.isPartOf | DRUG DEVELOPMENT AND INDUSTRIAL PHARMACY | - |
dc.rights | CC BY-NC-ND 2.0 KR | - |
dc.rights | https://creativecommons.org/licenses/by-nc-nd/2.0/kr/ | - |
dc.subject.MESH | Animals | - |
dc.subject.MESH | Antineoplastic Agents/chemistry | - |
dc.subject.MESH | Antineoplastic Agents/pharmacokinetics* | - |
dc.subject.MESH | Biological Availability* | - |
dc.subject.MESH | Chemistry, Pharmaceutical | - |
dc.subject.MESH | Erlotinib Hydrochloride/chemistry | - |
dc.subject.MESH | Erlotinib Hydrochloride/pharmacokinetics* | - |
dc.subject.MESH | Erlotinib Hydrochloride/pharmacology | - |
dc.subject.MESH | Excipients/chemistry* | - |
dc.subject.MESH | Humans | - |
dc.subject.MESH | Lung Neoplasms/drug therapy* | - |
dc.subject.MESH | Mice, Nude | - |
dc.subject.MESH | Nanoparticles/chemistry* | - |
dc.subject.MESH | Solubility | - |
dc.title | Nanoparticulation improves bioavailability of Erlotinib | - |
dc.type | Article | - |
dc.contributor.college | College of Medicine | - |
dc.contributor.department | Dept. of Biochemistry & Molecular Biology | - |
dc.contributor.googleauthor | Kyung Mi Yang | - |
dc.contributor.googleauthor | In Chul Shin | - |
dc.contributor.googleauthor | Joo Won Park | - |
dc.contributor.googleauthor | Kab-Sig Kim | - |
dc.contributor.googleauthor | Dae Kyong Kim | - |
dc.contributor.googleauthor | Kyungmoon Park | - |
dc.contributor.googleauthor | Kunhong Kim | - |
dc.identifier.doi | 10.1080/03639045.2017.1326931 | - |
dc.contributor.localId | A00289 | - |
dc.contributor.localId | A02279 | - |
dc.relation.journalcode | J03336 | - |
dc.identifier.eissn | 1520-5762 | - |
dc.identifier.pmid | 28554216 | - |
dc.identifier.url | https://www.tandfonline.com/doi/full/10.1080/03639045.2017.1326931 | - |
dc.subject.keyword | Bioavailability | - |
dc.subject.keyword | Erlotinib | - |
dc.subject.keyword | NUFS-Ert | - |
dc.subject.keyword | fed-fasted variance | - |
dc.subject.keyword | pharmacokinetics | - |
dc.contributor.alternativeName | Kim, Kun Hong | - |
dc.contributor.alternativeName | Yang, Kyung Mi | - |
dc.contributor.affiliatedAuthor | Kim, Kun Hong | - |
dc.contributor.affiliatedAuthor | Yang, Kyung Mi | - |
dc.citation.volume | 43 | - |
dc.citation.number | 9 | - |
dc.citation.startPage | 1557 | - |
dc.citation.endPage | 1565 | - |
dc.identifier.bibliographicCitation | DRUG DEVELOPMENT AND INDUSTRIAL PHARMACY, Vol.43(9) : 1557-1565, 2017 | - |
dc.identifier.rimsid | 61215 | - |
dc.type.rims | ART | - |
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