Evaluation of microporous polycaprolactone matrices for controlled delivery of antiviral microbicides to the female genital tract

Asvadi, Naghme Hajarol, Dang, Nhung T. T., Davis-Poynter, Nicholas and Coombes, Allan G. A. (2013) Evaluation of microporous polycaprolactone matrices for controlled delivery of antiviral microbicides to the female genital tract. Journal of Materials Science: Materials in Medicine, 24 12: 2719-2727. doi:10.1007/s10856-013-5010-6

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Author Asvadi, Naghme Hajarol
Dang, Nhung T. T.
Davis-Poynter, Nicholas
Coombes, Allan G. A.
Title Evaluation of microporous polycaprolactone matrices for controlled delivery of antiviral microbicides to the female genital tract
Journal name Journal of Materials Science: Materials in Medicine   Check publisher's open access policy
ISSN 0957-4530
1573-4838
Publication date 2013-12
Year available 2013
Sub-type Article (original research)
DOI 10.1007/s10856-013-5010-6
Volume 24
Issue 12
Start page 2719
End page 2727
Total pages 9
Place of publication New York, NY, United States
Publisher Springer New York
Collection year 2014
Language eng
Formatted abstract
Acyclovir (ACV) as a model antiviral microbicide, was incorporated in controlled-release polycaprolactone (PCL) matrices designed for application as intra-vaginal ring inserts (IVRs). Microporous materials incorporating acyclovir up to a level of ~10 % w/w were produced by rapidly cooling suspensions of drug powder in PCL solution followed by solvent extraction from the hardened matrices. Around 21, 50 and 78 % of the drug content was gradually released from matrices over 30 days in simulated vaginal fluid at 37 °C, corresponding to drug loadings of 5.9, 7.0 and 9.6 % w/w. The release behaviour of matrices having the lowest drug loading followed a zero order model, whereas, the release kinetics of 7.0 and 9.6 % ACV-loaded PCL matrices could be described effectively by the Higuchi model, suggesting that Fickian diffusion is controlling drug release. Corresponding values of the diffusion co-efficient for ACV in the PCL matrices of 3.16 × 10−9 and 1.07 × 10−8 cm2/s were calculated. Plaque reduction assays provided an IC50 value of 1.09 μg/mL for acyclovir against HSV-2 and confirmed the antiviral activity of released acyclovir against HSV-2 replication in primate kidney cells (Vero) at levels ~70 % that of non-formulated acyclovir at day 30. Estimated minimum in vivo acyclovir concentrations produced by a PCL IVR (19 μg/mL) exceeded by a factor of 20 the IC50 value against HSV-2 and the reported ACV vaginal concentrations in women (0.5–1.0 μg/mL) following oral administration. These findings recommend further investigations of PCL matrices for vaginal delivery of antiviral agents in the treatment and prevention of sexually transmitted infections such as AIDS.
Q-Index Code C1
Q-Index Status Confirmed Code
Institutional Status UQ
Additional Notes Published online: 28 July 2013.

Document type: Journal Article
Sub-type: Article (original research)
Collections: Official 2014 Collection
School of Pharmacy Publications
Clinical Medical Virology Centre Publications
 
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Citation counts: TR Web of Science Citation Count  Cited 7 times in Thomson Reuters Web of Science Article | Citations
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Created: Mon, 09 Sep 2013, 22:48:03 EST by Nhung Dang on behalf of School of Pharmacy