Nanoparticulation improves bioavailability of Erlotinib
DC Field | Value | Language |
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dc.contributor.author | Yang, Kyung Mi | - |
dc.contributor.author | Shin, In Chul | - |
dc.contributor.author | Park, Joo Won | - |
dc.contributor.author | Kim, Kab-Sig | - |
dc.contributor.author | Kim, Dae Kyong | - |
dc.contributor.author | Park, Kyungmoon | - |
dc.contributor.author | Kim, Kunhong | - |
dc.date.available | 2020-07-10T05:41:17Z | - |
dc.date.created | 2020-07-06 | - |
dc.date.issued | 2017 | - |
dc.identifier.issn | 0363-9045 | - |
dc.identifier.uri | https://scholarworks.bwise.kr/hongik/handle/2020.sw.hongik/6950 | - |
dc.description.abstract | Objectives: Nanoparticulation using fat and supercritical fluid (NUFS (TM)) 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 250nm and were stable for 2 months at 40 degrees C, 4 degrees 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 (R). In addition, experimental lung metastasis was more efficiently inhibited by NUFS-Ert than by Tarceva (R). The relative bioavailability of NUFS-Ert compared with that of Tarceva (R) 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 (R). Conclusions: NUFS-Ert could improve poor bioavailability and reduce fed-fasted bioavailability variances of Ert. NUFS-Ert was more efficacious than Tarceva (R). | - |
dc.language | 영어 | - |
dc.language.iso | en | - |
dc.publisher | TAYLOR & FRANCIS LTD | - |
dc.subject | CELL LUNG-CANCER | - |
dc.subject | RECEPTOR TYROSINE-KINASE | - |
dc.subject | IN-VITRO EVALUATION | - |
dc.subject | ORAL BIOAVAILABILITY | - |
dc.subject | HYBRID NANOPARTICLES | - |
dc.subject | INHIBITOR | - |
dc.subject | PHARMACOKINETICS | - |
dc.subject | DELIVERY | - |
dc.subject | THERAPY | - |
dc.subject | FORMULATION | - |
dc.title | Nanoparticulation improves bioavailability of Erlotinib | - |
dc.type | Article | - |
dc.contributor.affiliatedAuthor | Park, Kyungmoon | - |
dc.identifier.doi | 10.1080/03639045.2017.1326931 | - |
dc.identifier.scopusid | 2-s2.0-85019725014 | - |
dc.identifier.wosid | 000404797500018 | - |
dc.identifier.bibliographicCitation | DRUG DEVELOPMENT AND INDUSTRIAL PHARMACY, v.43, no.9, pp.1557 - 1565 | - |
dc.relation.isPartOf | DRUG DEVELOPMENT AND INDUSTRIAL PHARMACY | - |
dc.citation.title | DRUG DEVELOPMENT AND INDUSTRIAL PHARMACY | - |
dc.citation.volume | 43 | - |
dc.citation.number | 9 | - |
dc.citation.startPage | 1557 | - |
dc.citation.endPage | 1565 | - |
dc.type.rims | ART | - |
dc.type.docType | Article | - |
dc.description.journalClass | 1 | - |
dc.description.journalRegisteredClass | scie | - |
dc.description.journalRegisteredClass | scopus | - |
dc.relation.journalResearchArea | Pharmacology & Pharmacy | - |
dc.relation.journalWebOfScienceCategory | Chemistry, Medicinal | - |
dc.relation.journalWebOfScienceCategory | Pharmacology & Pharmacy | - |
dc.subject.keywordPlus | CELL LUNG-CANCER | - |
dc.subject.keywordPlus | RECEPTOR TYROSINE-KINASE | - |
dc.subject.keywordPlus | IN-VITRO EVALUATION | - |
dc.subject.keywordPlus | ORAL BIOAVAILABILITY | - |
dc.subject.keywordPlus | HYBRID NANOPARTICLES | - |
dc.subject.keywordPlus | INHIBITOR | - |
dc.subject.keywordPlus | PHARMACOKINETICS | - |
dc.subject.keywordPlus | DELIVERY | - |
dc.subject.keywordPlus | THERAPY | - |
dc.subject.keywordPlus | FORMULATION | - |
dc.subject.keywordAuthor | Bioavailability | - |
dc.subject.keywordAuthor | Erlotinib | - |
dc.subject.keywordAuthor | fed-fasted variance | - |
dc.subject.keywordAuthor | NUFS-Ert | - |
dc.subject.keywordAuthor | pharmacokinetics | - |
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