Skip to main content
  • AACR Publications
    • Cancer Discovery
    • Cancer Epidemiology, Biomarkers & Prevention
    • Cancer Immunology Research
    • Cancer Prevention Research
    • Cancer Research
    • Clinical Cancer Research
    • Molecular Cancer Research
    • Molecular Cancer Therapeutics

  • Register
  • Log in
Advertisement

Main menu

  • Home
  • About
    • The Journal
    • AACR Journals
    • Subscriptions
    • Permissions and Reprints
    • Reviewing
  • Articles
    • OnlineFirst
    • Current Issue
    • Past Issues
    • Focus on Computer Resources
    • 75th Anniversary
    • Meeting Abstracts
  • For Authors
    • Information for Authors
    • Author Services
    • Best of: Author Profiles
    • Submit
  • Alerts
    • Table of Contents
    • OnlineFirst
    • Editors' Picks
    • Citations
    • Author/Keyword
  • News
    • Cancer Discovery News
  • AACR Publications
    • Cancer Discovery
    • Cancer Epidemiology, Biomarkers & Prevention
    • Cancer Immunology Research
    • Cancer Prevention Research
    • Cancer Research
    • Clinical Cancer Research
    • Molecular Cancer Research
    • Molecular Cancer Therapeutics

User menu

  • Register
  • Log in

Search

  • Advanced search
Cancer Research
Cancer Research

Advanced Search

  • Home
  • About
    • The Journal
    • AACR Journals
    • Subscriptions
    • Permissions and Reprints
    • Reviewing
  • Articles
    • OnlineFirst
    • Current Issue
    • Past Issues
    • Focus on Computer Resources
    • 75th Anniversary
    • Meeting Abstracts
  • For Authors
    • Information for Authors
    • Author Services
    • Best of: Author Profiles
    • Submit
  • Alerts
    • Table of Contents
    • OnlineFirst
    • Editors' Picks
    • Citations
    • Author/Keyword
  • News
    • Cancer Discovery News
Experimental and Molecular Therapeutics

Comparative pharmacokinetics and biodistributions of mebendazole from cosolvent and nanoemulsion formulations in nude athymic mice

Yulan Qi, Pranav Gupta and Diana Chow
Yulan Qi
College of Pharmacy, University of Houston, Houston, TX
  • Find this author on Google Scholar
  • Find this author on PubMed
  • Search for this author on this site
Pranav Gupta
College of Pharmacy, University of Houston, Houston, TX
  • Find this author on Google Scholar
  • Find this author on PubMed
  • Search for this author on this site
Diana Chow
College of Pharmacy, University of Houston, Houston, TX
  • Find this author on Google Scholar
  • Find this author on PubMed
  • Search for this author on this site
DOI:  Published May 2007
  • Article
  • Info & Metrics
Loading
AACR Annual Meeting-- Apr 14-18, 2007; Los Angeles, CA

Abstract

2259

Objective: Mebendazole (Mbz), Methyl 5-benzoyl-2-benzimidazole carbamate, exerts growth inhibition in culture and tumor bearing nu/nu mice against NSCLC cell lines. The antineoplastic activity of MBZ is also evident in colorectal carcinoma and melanoma. A nanoemulsion (37 nm) formulation (PM1) of Mbz has been developed in our laboratory for potential parental delivery. This study was to comparatively characterize pharmacokinetics and biodistributions of Mbz from cosolvent formulation and PM1 in nude athymic mice.

Method: Mbz was administrated by i.v. bolus to the mice (30-35 gm) at 5 mg/kg for cosolvent system and 2.5 mg/kg for PM1. Concentrations of Mbz in plasma and five organs (heart, lung, liver, spleen, and kidney) were monitored by HPLC assays up to 6 hours post dose. The pharmacokinetic and tissue distribution profiles were constructed and pharmacokinetic parameters were derived using the WinNonlin.

Results: The plasma concentration-time profiles of Mbz from cosolvent and PM1 systems followed a two-compartment model with dose normalized AUCs of 2.46 and 2.38 μg·min/ml per μg dose, respectively. The clearance (CL) was 0.41 ml/min for cosolvent and 0.42 ml/min for PM1. The apparent volume distributions at steady-state (Vss) for cosolvent and PM1 were 42.8 ml and 38.8 ml, respectively. Different tissue distribution patterns between the two formulations were observed. For cosolvent, Mbz peak concentrations in different organs were reached in 5 minutes after injection. The highest peak concentration was 76.41 ng/g tissue/μg dose in liver, in contrast to 224.42 ng/g/μg in lung at 2 hr post dose for PM1. Mbz in cosolvent yielded the highest exposure in liver with AUC of 8.24 ug·min/g/ug dose, followed by kidney of 6.67 ug·min/g/ug. However, for PM1, AUC in lung (63.57 ug·min/g/ug) was the highest, which was about 20 folds of that from cosolvent (3.24 ug·min/g/ug), followed by those in liver (5.56 ug·min/g/ug) and kidney (5.22 ug·min/g/ug). For cosolvent, the elimination half-lives were 80, 72, 91, 84 and 98 min in heart, lung, liver, spleen, and kidney, respectively. For PM1, the elimination half-lives were substantially prolonged than those from cosolvent, 96, 172, 193, 123 and 131 min in heart, lung, liver, spleen, and kidney, respectively.

Conclusion: Mbz in cosolvent and PM1 systems exhibit similar plasma pharmacokinetics, but distinct tissue distributions. PM1 yields higher Mbz concentrations and prolonged exposures in organs than cosolvent, especially in lung, which may have potential value for lung cancer therapy.

Footnotes

  • 98th AACR Annual Meeting-- Apr 14-18, 2007; Los Angeles, CA

  • American Association for Cancer Research
Previous
Back to top
Cancer Research: 67 (9 Supplement)
May 2007
Volume 67, Issue 9 Supplement
  • Table of Contents
  • Index by Author

Sign up for alerts

Article Alerts
Sign In to Email Alerts with your Email Address
Email Article

Thank you for sharing this Cancer Research article.

NOTE: We request your email address only to inform the recipient that it was you who recommended this article, and that it is not junk mail. We do not retain these email addresses.

Enter multiple addresses on separate lines or separate them with commas.
Comparative pharmacokinetics and biodistributions of mebendazole from cosolvent and nanoemulsion formulations in nude athymic mice
(Your Name) has forwarded a page to you from Cancer Research
(Your Name) thought you would be interested in this article in Cancer Research.
Citation Tools
Comparative pharmacokinetics and biodistributions of mebendazole from cosolvent and nanoemulsion formulations in nude athymic mice
Yulan Qi, Pranav Gupta and Diana Chow
Cancer Res May 1 2007 (67) (9 Supplement) 2259;

Citation Manager Formats

  • BibTeX
  • Bookends
  • EasyBib
  • EndNote (tagged)
  • EndNote 8 (xml)
  • Medlars
  • Mendeley
  • Papers
  • RefWorks Tagged
  • Ref Manager
  • RIS
  • Zotero
Share
Comparative pharmacokinetics and biodistributions of mebendazole from cosolvent and nanoemulsion formulations in nude athymic mice
Yulan Qi, Pranav Gupta and Diana Chow
Cancer Res May 1 2007 (67) (9 Supplement) 2259;
del.icio.us logo Digg logo Reddit logo Twitter logo CiteULike logo Facebook logo Google logo Mendeley logo
  • Tweet Widget
  • Facebook Like
  • Google Plus One

Jump to section

  • Article
  • Info & Metrics
Advertisement

Related Articles

Cited By...

More in this TOC Section

Experimental and Molecular Therapeutics

  • Abstract SY14-03: Anaplastic lymphoma kinase (ALK): Normal biology and role in hematopoietic malignancies
  • Abstract SY18-01: Targeting the p53-MDM2 interaction for cancer therapy
  • Abstract SSY01-04: Discovery and validation of genome-wide genetic signatures of chemotherapy susceptibility: A translational model
Show more 3

Drug Delivery 2: Poster Presentations

  • Tolerability of an Investigational Electroporation Device, MedPulser™ DNA Delivery System (DDS) in Healthy Adults
  • Schedule-dependent enhancement of docetaxel by genistein combined polysaccharide (GCP) in prostate cancer
  • A thermally responsive Tat-elastin-like polypeptide fusion protein induces membrane leakage, apoptosis, and cell death in human breast cancer cells
Show more 3
  • Home
  • Alerts
  • Feedback
Facebook  Twitter  LinkedIn  YouTube  RSS

Articles

  • Online First
  • Current Issue
  • Past Issues
  • Meeting Abstracts

Info for

  • Authors
  • Subscribers
  • Advertisers
  • Librarians
  • Reviewers

About Cancer Research

  • About the Journal
  • Editorial Board
  • Permissions
  • Submit a Manuscript
AACR logo

Copyright © 2018 by the American Association for Cancer Research.

Cancer Research Online ISSN: 1538-7445
Cancer Research Print ISSN: 0008-5472
Journal of Cancer Research ISSN: 0099-7013
American Journal of Cancer ISSN: 0099-7374

Advertisement