0 160

Cited 6 times in

Nanoparticulation improves bioavailability of Erlotinib

DC FieldValueLanguage
dc.contributor.author김건홍-
dc.contributor.author양경미-
dc.date.accessioned2018-07-20T08:34:14Z-
dc.date.available2018-07-20T08:34:14Z-
dc.date.issued2017-
dc.identifier.issn0363-9045-
dc.identifier.urihttps://ir.ymlib.yonsei.ac.kr/handle/22282913/161293-
dc.description.abstractOBJECTIVES: 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.statementOfResponsibilityrestriction-
dc.languageEngland-
dc.publisher1520-5762-
dc.relation.isPartOfDRUG DEVELOPMENT AND INDUSTRIAL PHARMACY-
dc.rightsCC BY-NC-ND 2.0 KR-
dc.rightshttps://creativecommons.org/licenses/by-nc-nd/2.0/kr/-
dc.subject.MESHAnimals-
dc.subject.MESHAntineoplastic Agents/chemistry-
dc.subject.MESHAntineoplastic Agents/pharmacokinetics*-
dc.subject.MESHBiological Availability*-
dc.subject.MESHChemistry, Pharmaceutical-
dc.subject.MESHErlotinib Hydrochloride/chemistry-
dc.subject.MESHErlotinib Hydrochloride/pharmacokinetics*-
dc.subject.MESHErlotinib Hydrochloride/pharmacology-
dc.subject.MESHExcipients/chemistry*-
dc.subject.MESHHumans-
dc.subject.MESHLung Neoplasms/drug therapy*-
dc.subject.MESHMice, Nude-
dc.subject.MESHNanoparticles/chemistry*-
dc.subject.MESHSolubility-
dc.titleNanoparticulation improves bioavailability of Erlotinib-
dc.typeArticle-
dc.contributor.collegeCollege of Medicine-
dc.contributor.departmentDept. of Biochemistry & Molecular Biology-
dc.contributor.googleauthorKyung Mi Yang-
dc.contributor.googleauthorIn Chul Shin-
dc.contributor.googleauthorJoo Won Park-
dc.contributor.googleauthorKab-Sig Kim-
dc.contributor.googleauthorDae Kyong Kim-
dc.contributor.googleauthorKyungmoon Park-
dc.contributor.googleauthorKunhong Kim-
dc.identifier.doi10.1080/03639045.2017.1326931-
dc.contributor.localIdA00289-
dc.contributor.localIdA02279-
dc.relation.journalcodeJ03336-
dc.identifier.eissn1520-5762-
dc.identifier.pmid28554216-
dc.identifier.urlhttps://www.tandfonline.com/doi/full/10.1080/03639045.2017.1326931-
dc.subject.keywordBioavailability-
dc.subject.keywordErlotinib-
dc.subject.keywordNUFS-Ert-
dc.subject.keywordfed-fasted variance-
dc.subject.keywordpharmacokinetics-
dc.contributor.alternativeNameKim, Kun Hong-
dc.contributor.alternativeNameYang, Kyung Mi-
dc.contributor.affiliatedAuthorKim, Kun Hong-
dc.contributor.affiliatedAuthorYang, Kyung Mi-
dc.citation.volume43-
dc.citation.number9-
dc.citation.startPage1557-
dc.citation.endPage1565-
dc.identifier.bibliographicCitationDRUG DEVELOPMENT AND INDUSTRIAL PHARMACY, Vol.43(9) : 1557-1565, 2017-
Appears in Collections:
1. College of Medicine (의과대학) > Dept. of Biochemistry and Molecular Biology (생화학-분자생물학교실) > 1. Journal Papers

qrcode

Items in DSpace are protected by copyright, with all rights reserved, unless otherwise indicated.