Skip Navigation



JAC Advance Access published online on September 9, 2005
Journal of Antimicrobial Chemotherapy, doi:10.1093/jac/dki326
This Article
Right arrow FREE Full Text (PDF) Freely available
Right arrow All Versions of this Article:
56/5/954    most recent
dki326v1
Right arrow Alert me when this article is cited
Right arrow Alert me if a correction is posted
Services
Right arrow Email this article to a friend
Right arrow Similar articles in this journal
Right arrow Similar articles in PubMed
Right arrow Alert me to new issues of the journal
Right arrow Add to My Personal Archive
Right arrow Download to citation manager
Right arrowRequest Permissions
Right arrow Disclaimer
Google Scholar
Right arrow Articles by Malcolm, R. K.
Right arrow Articles by McCullagh, S. D.
Right arrow Search for Related Content
PubMed
Right arrow PubMed Citation
Right arrow Articles by Malcolm, R. K.
Right arrow Articles by McCullagh, S. D.
Social Bookmarking
Add to CiteULike   Add to Connotea   Add to Del.icio.us  
What's this?

© The Author 2005. Published by Oxford University Press on behalf of the British Society for Antimicrobial Chemotherapy. All rights reserved. For Permissions, please e-mail: journals.permissions@oxfordjournals.org
Received June 21, 2005
Revised August 17, 2005
Accepted August 17, 2005

Brief report

Long-term, controlled release of the HIV microbicide TMC120 from silicone elastomer vaginal rings

R. Karl Malcolm 1*, A. David Woolfson 1, Clare F. Toner 1, Ryan J. Morrow 1, and Stephen D. McCullagh 1

1 School of Pharmacy, Medical Biology Centre, Queen's University of Belfast, 97 Lisburn Road, Belfast BT9 7BL, Northern Ireland, UK

* To whom correspondence should be addressed.
R. Karl Malcolm, E-mail: k.malcolm{at}qub.ac.uk


  Abstract

Objectives: The feasibility of providing prolonged and controlled release of the experimental non-nucleoside reverse transcriptase inhibitor TMC120 from a silicone vaginal ring in quantities sufficient to maintain a vaginal concentration offering protection against heterosexual HIV transmission was investigated.

Methods: Core-type, silicone elastomer vaginal rings containing TMC120 were manufactured, and in vitro release studies performed under sink conditions. The experimental release data, as determined by HPLC, were correlated with estimates of vaginal TMC120 concentrations required to inhibit HIV replication.

Results: Continuous, zero-order release of TMC120 from core-type vaginal rings was observed in vitro over a 71 day period, equivalent to 136 µg/day. The release rate is predicted to maintain vaginal concentrations of the antiretroviral in the range of several orders of magnitude in excess of reported HIV inhibitory concentration values.

Conclusions: Continuous and prolonged zero-order release of TMC120 from a silicone vaginal ring device at quantities predicted to prevent HIV infection was observed.

Keywords: antiviral; diffusion; drug release; zero order.
Add to CiteULike CiteULike   Add to Connotea Connotea   Add to Del.icio.us Del.icio.us    What's this?


This article has been cited by other articles:


Home page
 Antimicrob. Agents Chemother.Home page
P. Fletcher, S. Harman, H. Azijn, N. Armanasco, P. Manlow, D. Perumal, M.-P. de Bethune, J. Nuttall, J. Romano, and R. Shattock
Inhibition of Human Immunodeficiency Virus Type 1 Infection by the Candidate Microbicide Dapivirine, a Nonnucleoside Reverse Transcriptase Inhibitor
Antimicrob. Agents Chemother., February 1, 2009; 53(2): 487 - 495.
[Abstract] [Full Text] [PDF]

Home page
 GlycobiologyHome page
T. Ghosh, K. Chattopadhyay, M. Marschall, P. Karmakar, P. Mandal, and B. Ray
Focus on antivirally active sulfated polysaccharides: From structure-activity analysis to clinical evaluation
Glycobiology, January 1, 2009; 19(1): 2 - 15.
[Abstract] [Full Text] [PDF]

Home page
 Proc. Natl. Acad. Sci. USAHome page
R. S. Veazey, T. A. Ketas, P. J. Klasse, D. K. Davison, M. Singletary, L. C. Green, M. L. Greenberg, and J. P. Moore
Tropism-independent protection of macaques against vaginal transmission of three SHIVs by the HIV-1 fusion inhibitor T-1249
PNAS, July 29, 2008; 105(30): 10531 - 10536.
[Abstract] [Full Text] [PDF]

Home page
 Proc. Natl. Acad. Sci. USAHome page
D. P. Wilson, P. M. Coplan, M. A. Wainberg, and S. M. Blower
The paradoxical effects of using antiretroviral-based microbicides to control HIV epidemics
PNAS, July 15, 2008; 105(28): 9835 - 9840.
[Abstract] [Full Text] [PDF]


Disclaimer: Please note that abstracts for content published before 1996 were created through digital scanning and may therefore not exactly replicate the text of the original print issues. All efforts have been made to ensure accuracy, but the Publisher will not be held responsible for any remaining inaccuracies. If you require any further clarification, please contact our Customer Services Department.