Hydrogels containing monocaprin have potent microbicidal activities against sexually transmitted viruses and bacteria in vitro

Thormar, Halldór; Bergsson, Gudmundur; Gunnarsson, Eggert; Georgsson, Guðmundur; Witvrouw, Myriam; Steingrı́msson, Ólafur; Clercq, Erik De; Kristmundsdóttir, Thórdís

doi:10.1136/sti.75.3.181

Cited by 60 publications

(49 citation statements)

References 24 publications

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“…Recent studies on the effect of fatty acids and monoglycerides on Chlamydia trachomatis 13 have shown that monocaprin is also the most active in killing this bacterium in a short time and that hydrogel formulations 1A, 1B, and 2A containing 10 mM monocaprin kill Chlamydis trachomatis and Neisseria gonorrheae at high titers in 5 and 1 min, respectively. 14 The hydrogel formulations in 10 -1 dilution were found to be toxic to monolayers of CV-1 cells, but they were 10-to 100-fold less cytotoxic than a commercial spermicidal product containing 2% nonoxynol-9. However, such a comparison must also be carried out in vivo.…”

Section: Discussionmentioning

confidence: 98%

Development and evaluation of microbicidal hydrogels containing monoglyceride as the active ingredient

Kristmundsdóttir

Árnadóttir

Bergsson

et al. 1999

Journal of Pharmaceutical Sciences

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A number of medium-chain saturated and long-chain unsaturated fatty acids and their monoglycerides were tested against herpes simplex virus (HSV-1) to determine which lipids were most active during a short incubation time. The aim was to find which lipid would be preferable as the active ingredient in a virucidal hydrogel formulation for the purpose of preventing transmission of pathogens to mucosal membranes, particularly sexually transmitted viruses, such as herpes simplex virus and human immunodeficiency virus (HIV), and bacteria, such as Chlamydia trachomatis and Neisseria gonorrheae. The main strategy was that the formulations would be fast-acting, killing large numbers of virus or bacteria on contact in a short time, preferably causing at least a 10000-fold reduction in virus/bacteria titer in 1-5 min. Monocaprin, the 1-monoglyceride of capric acid, and lauric acid were found to be most active of all the lipids tested, causing a greater than 100000-fold reduction in virus titer in 1 min at a concentration of 20 mM. When tested at a concentration of 10 mM for 1 min, monocaprin was still fully active whereas lauric acid had no or negligible activity. It was concluded that monocaprin was most suitable as the active ingredient in a fast-acting virucidal gel formulation, and several hydrogel formulations containing monocaprin were tested. Formulations where the monoglyceride was dissolved in glycofurol were found to be active against HSV-1. The hydrogel formulations containing 20 mM monocaprin were highly virucidal in vitro and caused a greater than 100000-fold (HSV-1) inactivation of virus in human semen in 1 min. Formulations in dilution 1:10 were cytotoxic in monolayers of CV-1 cells, but they were 10-100 fold less cytotoxic than a commercial product which contains 2% nonoxynol-9.

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Section: Discussionmentioning

confidence: 98%

Development and evaluation of microbicidal hydrogels containing monoglyceride as the active ingredient

Kristmundsdóttir

Árnadóttir

Bergsson

et al. 1999

Journal of Pharmaceutical Sciences

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“…In vitro studies have shown that monocaprin gels formulated using sodium carboxymethylcellulose and polyvinylpyrrolidone or carbomer and hydroxypropylmethylcellulose, are virucidal to HSV-1 and less cytotoxic than nonoxynol-9 (123). In vivo studies in mice showed that the gels were non-irritant and non-toxic in the vagina (122).…”

Section: A Monocaprin-loaded Hydrogel Formulationmentioning

confidence: 99%

A Review of Current Intravaginal Drug Delivery Approaches Employed for the Prophylaxis of HIV/AIDS and Prevention of Sexually Transmitted Infections

et al. 2008

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Abstract. The objective of this review is to describe the current status of several intravaginal anti-HIV microbicidal delivery systems these delivery systems and microbicidal compounds in the context of their stage within clinical trials and their potential cervicovaginal defence successes. The global Human Immuno-Deficiency Virus (HIV) pandemic continues to spread at a rate of more than 15,000 new infections daily and sexually transmitted infections (STIs) can predispose people to acquiring HIV infection. Male-to-female transmission is eight times more likely to occur than female-to-male transmission due to the anatomical structure of the vagina as well as socio-economic factors and the disempowerment of women that renders them unable to refuse unsafe sexual practices in some communities. The increased incidence of HIV in women has identified the urgent need for efficacious and safe intravaginal delivery of anti-HIV agents that can be used and controlled by women. To meet this challenge, several intravaginal anti-HIV microbicidal delivery systems are in the process of been developed. The outcomes of three main categories are discussed in this review: namely, dual-function polymeric systems, non-polymeric systems and nanotechnology-based systems. These delivery systems include formulations that modify the genital environment (e.g. polyacrylic acid gels and lactobacillus gels), surfactants (e.g. sodium lauryl sulfate), polyanionic therapeutic polymers (e.g. carageenan and carbomer/lactic acid gels), proteins (e.g. cyanovirin-N, monoclonal antibodies and thromspondin-1 peptides), protease inhibitors and other molecules (e.g. dendrimer based-gels and the molecular condom). Intravaginal microbicide delivery systems are providing a new option for preventing the transmission of STIs and HIV.

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“…Even if lipids are toxic in cell cultures, studies have shown that they are not toxic to skin and mucosa at much higher concentrations. Thus, hydrogels containing monocaprin at a concentration of 5 mg/ml (20 mM) have been shown not to cause irritation of the vaginal mucosas of mice and rabbits (13) or the skin of hairless mice (9).…”

Section: ϫ6mentioning

confidence: 99%

In Vitro Killing of Candida albicans by Fatty Acids and Monoglycerides

Bergsson

Arnfinnsson

Steingrı́msson

et al. 2001

Antimicrob Agents Chemother

257

187

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The susceptibility of Candida albicans to several fatty acids and their 1-monoglycerides was tested with a short inactivation time, and ultrathin sections were studied by transmission electron microscopy (TEM) after treatment with capric acid. The results show that capric acid, a 10-carbon saturated fatty acid, causes the fastest and most effective killing of all three strains of C. albicans tested, leaving the cytoplasm disorganized and shrunken because of a disrupted or disintegrated plasma membrane. Lauric acid, a 12-carbon saturated fatty acid, was the most active at lower concentrations and after a longer incubation time.

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Hydrogels containing monocaprin have potent microbicidal activities against sexually transmitted viruses and bacteria in vitro

Cited by 60 publications

References 24 publications

Development and evaluation of microbicidal hydrogels containing monoglyceride as the active ingredient

Development and evaluation of microbicidal hydrogels containing monoglyceride as the active ingredient

A Review of Current Intravaginal Drug Delivery Approaches Employed for the Prophylaxis of HIV/AIDS and Prevention of Sexually Transmitted Infections

In Vitro Killing of Candida albicans by Fatty Acids and Monoglycerides

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