ArticleAntimicrobial agents and chemotherapy2010
In vitro evaluation of viability, integrity, and inflammation in genital epithelia upon exposure to pharmaceutical excipients and candidate microbicides.
Article in Antimicrobial agents and chemotherapy, 2010. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 20 papers.
What it found
Each row is one number read from the abstract, on the scale the paper reported it, with its interval. Left of the dashed line favours the treatment, right favours the comparator. Under each row is the sentence it came from. New to these charts? A ten-minute tutorial.
The abstract states no effect estimate the extractor could read, or names no intervention and outcome on the map, so this paper lights no cell and moves no belief. It is still indexed, cited and linked below.
The trial behind it
Trials whose registry record cites this paper, or whose number appears in the abstract. A trial that started after this paper was published is citing it as background, not reporting it.
Neither the registry nor the abstract names a trial number. If this is a trial report, that itself is worth knowing.
Who cites it
20 citing papers in PubMed, 67 citations in OpenAlex.
- Vaginal Sheets withGels (Basel, Switzerland) · 2023Article
- Advanced Solid Formulations For Vulvovaginal Candidiasis.Pharmaceutical research · 2023Review
- In vitro and ex vivo models for evaluating vaginal drug delivery systems.Advanced drug delivery reviews · 2022Review
- Comprehensive Study of Antiretroviral Drug Permeability at the Cervicovaginal MucosaPharmaceutics · 2022Article
- Baseline and time-updated factors in preclinical development of anionic dendrimers as successful anti-HIV-1 vaginal microbicides.Wiley interdisciplinary reviews. Nanomedicine and nanobiotechnology · 2022Review
- In vitro anti-HIV activity of some Indian medicinal plant extracts.BMC complementary medicine and therapies · 2020Article
- Reciprocal Modulation of Antiretroviral Drug and Steroid Receptor FunctionAntimicrobial agents and chemotherapy · 2019Article
- The Clinical Use of Monolaurin as a Dietary Supplement: A Review of the Literature.Journal of chiropractic medicine · 2019Article
- Rational Development of Liposomal Hydrogels: A Strategy for Topical Vaginal Antiretroviral Drug Delivery in the Context of HIV Prevention.Pharmaceutics · 2019Article
- Glycerol monolaurate nanocapsules for biomedical applications: in vitro toxicological studies.Naunyn-Schmiedeberg's archives of pharmacology · 2019Article
- [PSB0739 inhibits formation of semen-derived amyloid fibril].Nan fang yi ke da xue xue bao = Journal of Southern Medical University · 2018Article
- On-demand microbicide products: design matters.Drug delivery and translational research · 2017Review
- Impact of Hydroxychloroquine-Loaded Polyurethane Intravaginal Rings on Lactobacilli.Antimicrobial agents and chemotherapy · 2015Article
- Expression of Genes for Drug Transporters in the Human Female Genital Tract and Modulatory Effect of Antiretroviral Drugs.PloS one · 2015Article
- Characterization of commercially available vaginal lubricants: a safety perspective.Pharmaceutics · 2014Article
- Preformulation studies of EFdA, a novel nucleoside reverse transcriptase inhibitor for HIV prevention.Drug development and industrial pharmacy · 2014Article
- Human immunodeficiency virus and heparan sulfate: from attachment to entry inhibition.Frontiers in immunology · 2013Review
- Polymeric nanoparticles affect the intracellular delivery, antiretroviral activity and cytotoxicity of the microbicide drug candidate dapivirine.Pharmaceutical research · 2012Article
- Article
- The Effect of Commonly Used Excipients on the Epithelial Integrity of Human Cervicovaginal Tissue.AIDS research and human retrovirusesArticle
Corrections and comments
PubMed lists nothing against this paper. Absence here is not a guarantee, only a check that was made.
Authors and funding
10 authors at 3 institutions in 2 countries.
Funding
No grant is acknowledged in the PubMed record.
Abstract
The use of microbicides is a promising approach for the prevention of HIV-1 transmission. Unfortunately, various candidates failed in clinical trials. In some cases, the candidate microbicide even resulted in enhanced virus transmission. Therefore, there is an urgent need to develop more predictive preclinical strategies to anticipate the in vivo efficiency/toxicity rate, including in vitro assays that evaluate effects on epithelial integrity and inflammation. The present study aims to identify potential safety issues concerning the use of microbicides and excipients commonly used in vaginal microbicide preparations. The toxicities of various active pharmaceutical ingredients (APIs; TMC-120, UC-781, tenofovir [PMPA], PRO-2000, and glycerol monolaurate [GML]) and excipients (preservatives, cosolvents, surfactants, and cyclodextrins) were evaluated using an in vitro dual-chamber model and uterine cervical explants. Epithelial viability and permeation of fluorescent virus-sized beads, as well as induction of interleukin-8 (IL-8; as a sensitive marker of an inflammatory response), were assessed. Surprisingly, cell viability and epithelial layer integrity were compromised by most excipients at concentrations near the typical concentration used in vaginal gels, and a significant increase in the production of IL-8 was observed at subtoxic concentrations. Within the APIs, TMC-120, UC-781, and PMPA showed higher selectivity indices than PRO-2000 and GML. In conclusion, identification of safety issues concerning the use of pharmaceutical excipients could help to formulate less toxic vaginal microbicide preparations.
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Registered trials
Read under generation 80e0d062 · epoch 390. Bibliography from PubMed, PubMed Central and OpenAlex; grants from NIH RePORTER; trial links from ClinicalTrials.gov; estimates, votes and beliefs from the OpenQuestion graph.