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JAC Advance Access originally published online on September 9, 2005
Journal of Antimicrobial Chemotherapy 2005 56(5):954-956; doi:10.1093/jac/dki326
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© 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

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

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

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

Received 21 June 2005; returned 12 August 2005; revised 17 August 2005; accepted 17 August 2005

* Corresponding author. Tel: +44-28-9097-2319; Fax: +44-28-9024-7794; E-mail: k.malcolm{at}qub.ac.uk

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


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