Distribution of a vaginal gel (Invisible Condom®) before, during and after simulated sexual intercourse and its persistence when delivered by two different vaginal applicators: a magnetic resonance imaging study

Omar, Rabeea F.; Trottier, Sylvie; Brousseau, Ghislain; Lamarre, André; Gagnon, Alexandre; Bergeron, Michel G.

doi:10.1016/j.contraception.2008.01.015

Cited by 17 publications

(9 citation statements)

References 18 publications

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“…For example, many vaginal spermicides provide protection for no more than 1 h (40). Other vaginal products are not well-retained even after 6 h (7-9), necessitating repeated administration for adequate protection. Similarly, over 90% of CPs were shed from the vagina within 6 h because they did not penetrate deep into the mucus layers.…”

Section: Discussionmentioning

confidence: 99%

“…Additionally, to increase user acceptability, drug delivered to the vagina should be retained in the vaginal tract at effective concentrations over extended periods of time. Achieving sustained local drug concentrations is challenging because the vaginal epithelium is highly permeable to small molecules (10) and also because soluble drug dosage forms (gels, creams) can be expelled by intra-abdominal pressure and ambulation (7, 9). Lastly, drug delivery methods must be safe and non-toxic to the vaginal epithelium.…”

Section: Introductionmentioning

confidence: 99%

“…Poor distribution into the vaginal folds, even after simulated intercourse, has been cited as a critical factor for failure to protect susceptible vaginal surfaces from infection (4). Distribution over the entire susceptible target surface has been proven important for preventing and treating infections (5)(6)(7)(8)(9). Additionally, to increase user acceptability, drug delivered to the vagina should be retained in the vaginal tract at effective concentrations over extended periods of time.…”

Section: Introductionmentioning

confidence: 99%

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Mucus-Penetrating Nanoparticles for Vaginal Drug Delivery Protect Against Herpes Simplex Virus

et al. 2012

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Incomplete coverage and short duration of action limit the effectiveness of vaginally administered drugs, including microbicides for preventing sexually transmitted infections. We investigated vaginal distribution, retention, and safety of nanoparticles with surfaces modified to enhance transport through mucus. We show that mucus-penetrating particles (MPPs) provide uniform distribution over the vaginal epithelium, whereas conventional nanoparticles (CPs) that are mucoadhesive are aggregated by mouse vaginal mucus, leading to poor distribution. Moreover, when delivered hypotonically, MPPs were transported advectively (versus diffusively) through mucus deep into vaginal folds (rugae) within minutes. By penetrating into the deepest mucus layers, more MPPs were retained in the vaginal tract after 6 h compared to CPs. After 24 h, when delivered in a conventional vaginal gel, patches of a model drug remained on the vaginal epithelium, whereas the epithelium was coated with drug delivered by MPP. We then developed MPPs composed of acyclovir monophosphate (ACVp). When administered prior to vaginal herpes simplex virus 2 (HSV-2) challenge, ACVp-MPPs protected 53% of mice, compared to only 16% protected by soluble drug. Overall, MPPs improved vaginal drug distribution and retention, provided more effective protection against vaginal viral challenge than soluble drug, and were non-toxic when administered daily for one week.

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Section: Discussionmentioning

confidence: 99%

Section: Introductionmentioning

confidence: 99%

Section: Introductionmentioning

confidence: 99%

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Mucus-Penetrating Nanoparticles for Vaginal Drug Delivery Protect Against Herpes Simplex Virus

et al. 2012

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“…Omar et al [71] designed an applicator with multiple openings which aids spreading of gel in the vagina. This applicator was investigated for use in a spermicide product, the "Invisible Condom®" [72].…”

Section: Applicators For Vaginal Gelsmentioning

confidence: 99%

Polymeric gels for intravaginal drug delivery

Cook

Brown

2018

Journal of Controlled Release

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Intravaginal drug delivery can elicit a local effect, or deliver drugs systemically without hepatic first pass metabolism. There are a number of emerging areas in intravaginal drug delivery, but the vagina is a challenging route of administration, due to the clearance mechanisms present which result in poor retention of dosage forms, and the potential for irritation and other adverse reactions. Gel formulations are desirable due to the ease of application, spreading and that they cause little to no discomfort to the patient. However, these dosage forms, in particular, are poorly retained and traditional gels typically have little control over drug release rates. This has led to a large number of studies on improving the retention of vaginal gels and modulating the controlled release of drugs from the gel matrix. This review outlines the anatomy and physiology of the vagina, focussing on areas relevant to drug delivery. Medical applications of vaginally administered medicines is then discussed, followed by an overview of polymeric gels in intravaginal drug delivery. The sensorial properties of intravaginal gels, and how these relate to user compliance are also summarised. Finally, some important barriers to marketing approval are described.

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“…These results suggest the physical act of sexual intercourse results in mixing and dispersal of the microbicide product resulting in reduced effectiveness of a topical microbicide, and these factors should be evaluated during early product development. Instrumentation and methodology to perform studies to evaluate gel spreading and overall epithelium coverage within the vagina and rectum have been developed and employed to evaluate microbicide products in the context of coitus, and these evaluations will help to determine if a microbicide product is able to be in the right place and right concentration to prevent infection prior to and following coital events [29–31]. Confocal Raman spectroscopy (CRS) has recently been utilized to measure local concentrations of APIs in three dimensions in vaginal or rectal fluids, gels, and tissue explants, and this methodology may yield highly relevant data regarding the penetration of API into vaginal and rectal tissue [32].…”

Section: The Role Of the Complex Biological Environmentmentioning

confidence: 99%

Factors Important to the Prioritization and Development of Successful Topical Microbicides for HIV-1

Buckheit

2012

Molecular Biology International

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Significant advancements in topical microbicide development have occurred since the prevention strategy was first described as a means to inhibit the sexual transmission of HIV-1. The lack of clinical efficacy of the first generation microbicide products has focused development attention on specific antiretroviral agents, and these agents have proven partially successful in human clinical trials. With greater understanding of vaginal and rectal virus infection, replication, and dissemination, better microbicide products and delivery strategies should result in products with enhanced potency. However, a variety of development gaps exist which relate to product dosing, formulation and delivery, and pharmacokinetics and pharmacodynamics which must be better understood in order to prioritize microbicide products for clinical development. In vitro, ex vivo, and in vivo models must be optimized with regard to these development gaps in order to put the right product at the right place, at the right time, and at the right concentration for effective inhibition of virus transmission. As the microbicide field continues to evolve, we must harness the knowledge gained from unsuccessful and successful clinical trials and development programs to continuously enhance our preclinical development algorithms.

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Distribution of a vaginal gel (Invisible Condom®) before, during and after simulated sexual intercourse and its persistence when delivered by two different vaginal applicators: a magnetic resonance imaging study

Cited by 17 publications

References 18 publications

Mucus-Penetrating Nanoparticles for Vaginal Drug Delivery Protect Against Herpes Simplex Virus

Mucus-Penetrating Nanoparticles for Vaginal Drug Delivery Protect Against Herpes Simplex Virus

Polymeric gels for intravaginal drug delivery

Factors Important to the Prioritization and Development of Successful Topical Microbicides for HIV-1

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