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Results for “Spermicidal Contraceptive Agents”

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At least 19 recordsLinked to original sources
PubMed1996

Comparative in vitro spermicidal activity of chelating agents and synergistic effect with nonoxynol-9 on human sperm functionality.

Nonoxynol-9 (N-9), a nonionic surfactant, exerts both spermicidal and anti-viral activities and is the most widely used spermicide. Although N-9 has been regarded as an efficient spermicidal agent for barrier contraception, it has been reported to cause vaginal irritation and allergic vaginitis, and its spermicidal action in the vaginal mucus may be limited. To address these problems, the spermicidal activity of several chelating agents against human semen and their synergistic effect on the spermicidal activity of N-9 were evaluated using computer-assisted semen analysis and a cervical mucus penetration test. Carbopol 934P, chosen as a polymer base for dispersion of N-9 and chelating agent, was also evaluated for its potential spermicidal activity. Chelating agents, such as ethylenediaminetetraacetic acid (EDTA), ethylene bis(oxyethylenenitrilo)tetraacetic acid, and gramicidin, had spermicidal activity against human sperm at the tested concentration range and exerted spermicidal activity within mucus, impeding sperm penetration to the extended cervical space. A synergistic effect was shown between N-9 and EDTA on sperm motility. In dose-response curves, 0.1% EDTA significantly increased binding affinity constant and spermicidal potency of N-9 and reduced the concentration of N-9 at which 50% of the maximum response was observed from 144.5 to 66.4 (micrograms/mL). A synergistic effect was also shown between EDTA and carbopol 934P polymer on inhibition of sperm penetration through the cervical mucus. Therefore, EDTA can be used as a supplementary agent and potentiator for N-9. Development of a carbopol 934P-based drug delivery system for dual controlled release of N-9 in combination with chelating agents seems to be a promising approach for increasing the efficacy of fertility control.

Animals↗
PubMed1996

Synergistic effect of gramicidin and EDTA in inhibiting sperm motility and cervical mucus penetration in vitro.

Gramicidin, a linear polypeptide with antiviral and antimicrobial properties, was compared in vitro with a commonly used spermicidal detergent-nonoxynol-9 (N9). The inhibition of sperm functions was evaluated by computer-assisted semen analysis (CASA) for sperm motility, in cervical mucus penetration assay, and by colorimetric tetrazolium salt and lactate dehydrogenase release assays routinely employed for testing the toxicity of drugs. The effective 100% inhibitory concentration (IC100) of gramicidin in a 2-min sperm immobilization assay by CASA was equal to 4 micrograms/ml, whereas IC100 of N9 was equal to 200 micrograms/ml. The presence of 0.1% of chelating agent, EDTA, reduced IC100 of gramicidin to 10 ng/ml, while less than a twofold enhancement in N9 activity was observed upon combination with EDTA. Likewise, the gramicidin/EDTA combination was 100,000 times more potent than N9/EDTA in the sperm penetration assay. Quantitative toxicity tests confirmed that gramicidin is a potent spermostatic rather than spermicidal agent. Further development of a gramicidin/EDTA formulation is warranted as a nontoxic topical contraceptive with activity against viral and microbial sexually transmitted diseases (STDs).

Cervix Mucus↗
PubMed1982

Influence of lipid solubility on the sperm immobilizing effect of beta-adrenoceptor blocking drugs.

1 Sperm immobilizing effects of five beta-adrenoceptor blockers were measured on six human semen samples with a trans-membrane migration method. 2 The concentrations which decreased sperm motility to 50% of control (ED50) were 0.8, 4.2, 6.2, 11.0 and 33.0 mM for propranolol, oxprenolol, metoprolol, acebutolol and sotalol respectively. 3 There was a linear correlation between the log values of ED50 and the log partition coefficients of these beta-adrenoceptor blockers. 4 Because the lipid solubility determines the sperm immobilizing potencies of beta-adrenoceptor blockers, we support the theory that beta-adrenoceptor blockers inhibit sperm motility by stabilizing the cellular membrane. 5 The clinical implication of this finding is that more lipid soluble drugs are likely to have more interference on sperm function, at least when they are used locally.

Adrenergic beta-Antagonists↗
PubMed1987

The spermicidal potency of Coca-Cola and Pepsi-Cola.

The inhibitory effect of Old Coke, caffeine-free New Coke, New Coke, Diet Coke and Pepsi-Cola on human sperm motility was studied with a trans-membrane migration method. None of them could decrease sperm motility to less than 70% of control within one hour. A previous study which claimed a marked variation of spermicidal potencies among different formulations of Coca-Cola could not be confirmed. Even if cola has a spermicidal effect, its potency is relatively weak as compared with other well-known spermicidal agents.

Beverages↗
PubMed1992

Quantification of the in vitro activity of some compounds with spermicidal activity.

The in vitro spermicidal activity of the commonly used surfactant spermicides and the antiseptic chlorhexidine, were quantified in a statistically reproducible manner, using donor semen and image capture analysis. The spermicidal activity was expressed as the ED50 under defined assay conditions. Using these parameters, the order of spermicidal activity was: Menfegol > nonoxynol-9 approximately benzalkonium chloride > sodium docusate > chlorhexidine. These differences were statistically significant.

Benzalkonium Compounds↗