ArticleInternational journal of pharmaceutics2014
Development of a vaginal delivery film containing EFdA, a novel anti-HIV nucleoside reverse transcriptase inhibitor.
Article in International journal of pharmaceutics, 2014. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 14 papers.
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Who cites it
14 citing papers in PubMed, 39 citations in OpenAlex.
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- Development and Characterization of Mucoadhesive Films Containing Metronidazole for Vaginal Drug Delivery.Turkish journal of pharmaceutical sciences · 2025Article
- Development and Optimization of Oral Dissolution Films for Enhanced Delivery of Ebastine-Loaded Solid Lipid Nanoparticles.International journal of nanomedicine · 2025Article
- Vaginal Sheets withGels (Basel, Switzerland) · 2023Article
- Recent Advances in Polymer-Based Vaginal Drug Delivery Systems.Pharmaceutics · 2021Review
- Rational Design of a Multipurpose Bioadhesive Vaginal Film for Co-Delivery of Dapivirine and Levonorgestrel.Pharmaceutics · 2019Article
- Long-Acting Anti-HIV Drugs Targeting HIV-1 Reverse Transcriptase and Integrase.Pharmaceuticals (Basel, Switzerland) · 2019Review
- 4'-Ethynyl-2-fluoro-2'-deoxyadenosine, MK-8591: a novel HIV-1 reverse transcriptase translocation inhibitor.Current opinion in HIV and AIDS · 2018Review
- Long acting systemic HIV pre-exposure prophylaxis: an examination of the field.Drug delivery and translational research · 2017Review
- On-demand microbicide products: design matters.Drug delivery and translational research · 2017Review
- Historical development of vaginal microbicides to prevent sexual transmission of HIV in women: from past failures to future hopes.Drug design, development and therapy · 2017Review
- Vaginal Microbicide Film Combinations of Two Reverse Transcriptase Inhibitors, EFdA and CSIC, for the Prevention of HIV-1 Sexual Transmission.Pharmaceutical research · 2015Article
- Formulation, development and characterization of mucoadhesive film for treatment of vaginal candidiasis.International journal of pharmaceutical investigationArticle
Corrections and comments
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Authors and funding
5 authors at 3 institutions in 1 country.
Funding
Abstract
The aim of this work was to develop a fast-dissolving film formulation containing EFdA for potential use as a topical vaginal microbicide for prevention of HIV sexual transmission. Solid state compatibility approaches were used to screen commonly used polymers for formulation development. Factorial design and desirability function were used to investigate the effect of two variables, the ratio of the polymers and the concentration of selected plasticizer on four mechanical responses including tensile strength, elongation at break, toughness and elastic modulus for optimization of the film formulation. Assessments of EFdA-loaded films included physicochemical characteristics, in vitro cytotoxicity, epithelia integrity, ex vivo permeability and bioactivity test. The optimal placebo film was composed of PVA, HPMC E5 and propylene glycol (7:3:3, w/w), and its mechanical characteristics were comparable to those of VCF(®) film (a commercial vaginal film product). Permeability studies using human ectocervical explants showed that there was no significant difference in cumulative permeated amount of EFdA between EFdA film and free EFdA. The results of in vitro cytotoxicity and bioactivity testing showed that 50% cytotoxic concentration (CC50) was several orders of magnitude higher than 50% effective concentration (EC50) of EFdA. Furthermore, epithelial integrity study showed that EFdA-loaded film had a much lower toxicity to HEC-1A cell monolayers as compared to VCF(®). Therefore, EFdA-loaded vaginal film may be considered as a promising vaginal microbicide for HIV prevention.
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