ArticleThe Journal of antimicrobial chemotherapy2012
Safety and pharmacokinetics of aciclovir in women following release from a silicone elastomer vaginal ring.
Article in The Journal of antimicrobial chemotherapy, 2012. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 17 papers.
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Who cites it
17 citing papers in PubMed, 23 citations in OpenAlex.
- An intravaginal ring for HIV pre-exposure prophylaxis: assessment of safety and pharmacokinetics in a randomized, placebo-controlled clinical trial.Frontiers in cellular and infection microbiology · 2026Trial
- Trial
- Electrohydrodynamic Coating with Acyclovir PLGA Conjugate for Antiviral Functionalization of Medical Surfaces.International journal of molecular sciences · 2025Article
- The Vaginal Microbiota, Bacterial Biofilms and Polymeric Drug-Releasing Vaginal Rings.Pharmaceutics · 2021Review
- Vaginal rings with exposed cores for sustained delivery of the HIV CCR5 inhibitor 5P12-RANTES.Journal of controlled release : official journal of the Controlled Release Society · 2019Article
- Article
- Article
- Accurate measurement of female genital tract fluid dilution in cervicovaginal lavage samples.Journal of chromatography. B, Analytical technologies in the biomedical and life sciences · 2016Article
- Biomarkers and biometric measures of adherence to use of ARV-based vaginal rings.Journal of the International AIDS Society · 2016Review
- An intravaginal ring for the sustained delivery of antibodies.Journal of pharmaceutical sciences · 2014Article
- Comparison of the vaginal microbial communities in women with recurrent genital HSV receiving acyclovir intravaginal rings.Antiviral research · 2014Article
- Microbicides for the Treatment of Sexually Transmitted HIV Infections.Journal of pharmaceutics · 2014Review
- Experimental approaches to investigating the vaginal biofilm microbiome.Methods in molecular biology (Clifton, N.J.) · 2014Article
- Sustained delivery of commensal bacteria from pod-intravaginal rings.Antimicrobial agents and chemotherapy · 2014Article
- Changes in the soluble mucosal immune environment during genital herpes outbreaks.Journal of acquired immune deficiency syndromes (1999) · 2012Article
- An intravaginal ring for the simultaneous delivery of multiple drugs.Journal of pharmaceutical sciences · 2012Article
- Vaginal rings for delivery of HIV microbicides.International journal of women's health · 2012Article
Corrections and comments
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Authors and funding
15 authors at 5 institutions in 1 country.
Funding
Abstract
objectivesSystemic aciclovir and its prodrug valaciclovir are effective in treating and reducing recurrences of genital herpes simplex virus (HSV) and reducing transmission. Local aciclovir delivery, if it can achieve and maintain comparable intracellular genital tract levels, may be equally effective in the treatment and suppression of genital HSV. Intravaginal ring (IVR) delivery of aciclovir may provide pre-exposure prophylaxis against HSV acquisition.
methodsTolerability and pharmacokinetics were evaluated in six HIV-negative women with recurrent genital HSV who switched their daily oral valaciclovir suppression to an aciclovir IVR for 7 days (n = 3) or 14 days (n = 3). Blood and cervicovaginal lavage (CVL) were collected after oral and IVR dosing to measure aciclovir concentrations and genital swabs were obtained to quantify HSV shedding by PCR.
resultsThe rings were well tolerated. Median plasma aciclovir concentrations were 110.2 ng/mL (IQR, 85.9-233.5) 12-18 h after oral valaciclovir. Little or no drug was detected in plasma following IVR dosing. Median (IQR) CVL aciclovir levels were 127.3 ng/mL (21-660.8) 2 h after oral valaciclovir, 154.4 ng/mL (60.7-327.5) 12-18 h after oral valaciclovir and 438 ng/mL (178.5-618.5) after 7 days and 393 ng/mL (31.6-1615) after 14 days of aciclovir ring use. Median CVL aciclovir levels 2 h after oral dosing were similar to levels observed 7 (P = 0.99) and 14 (P = 0.75) days after ring use. HSV DNA was not detected in genital swabs and there was no significant change in inflammatory mediators.
conclusionsThis first-in-human study demonstrated that an IVR could safely deliver mucosal levels of aciclovir similar to oral valaciclovir without systemic absorption. More intensive site-specific pharmacokinetic studies are needed to determine whether higher local concentrations are needed to achieve optimal drug distribution within the genital tract.
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