Nonoxynol-9

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George A. Digenis - One of the best experts on this subject based on the ideXlab platform.

  • Synthesis of novel iodinated derivatives of Nonoxynol-9 and their bioavailability in rats
    Nuclear medicine and biology, 2002
    Co-Authors: Philip T. Fowler, Kazuya Matsumoto, Richard C. Page, George A. Digenis
    Abstract:

    The absorption and distribution of iodinated derivatives of Nonoxynol-9, after vaginal administration in rats, were compared with results reported for [14C] Nonoxynol-9. Mono-iodinated Nonoxynol-9 was synthesized in addition to the radiolabeled derivative incorporating iodide-125 ([125I]). Six hours after dosing, test rats were euthanized and selected tissues were excised and assessed for radioactivity. Levels of radioactive markers in the reproductive system were substantial for both [14C] and [125I]. It was concluded that [125I] mono-iodinated Nonoxynol-9 and [14C] Nonoxynol-9 possessed similar bioavailability.

  • Assessment of new formulations of Nonoxynol-9 coprecipitated with polyvinylpyrrolidone and iodine as possible vaginal contraceptives
    Fertility and sterility, 1996
    Co-Authors: Panayiotis M Zavos, Juan R. Correa, Dagmar Nosek, Fatemeh Mohammadi, George A. Digenis
    Abstract:

    Objective To assess the in vitro spermicidal activity of new formulations of Nonoxynol-9, coprecipitated with polyvinylpyrrolidone (PVP) or iodinated PVP, against human spermatozoa via the use of the Sander-Cramer test and the cervical mucus penetration test. Design Solutions of PVP-Nonoxynol-9 and iodinated PVP-Nonoxynol-9 containing Nonoxynol-9 whole molecule (oligomers 1 to 18) and its isolated fractions (oligomers 8 to 10, 4 to 6, and 1 to 3) at various concentrations ( μ g/mL) were prepared via serial dilutions. Spermicidal solutions were mixed with human semen to determine the minimal lethal dose ( μ g/mL). In the Sander-Cramer test, the lethal dose was reported as the minimal dose capable of killing spermatozoa within 20 seconds. In the cervical mucus penetration test, the lethal dose was reported as the minimal dose capable of preventing penetration of spermatozoa into cervical mucus beyond the second millimeter length of the capillary. Setting Andrology laboratory, University of Kentucky, Lexington, Kentucky. Patient(s) Normospermic male donors. Main Outcome Measure(s) Spermicidal lethal dose determination of various Nonoxynol-9 preparations containing the whole Nonoxynol-9 molecule and its isolated fractions coprecipitated with PVP or iodinated PVP. Result(s) The use of PVP increased the aqueous solubility of the Nonoxynol-9 formulations containing oligomers 1 to 18 and 8 to 10 slightly. The coprecipitation of the Nonoxynol-9 formulations containing Nonoxynol-9 oligomers 4 to 6 and 1 to 3 with PVP significantly increased their solubilization and spermicidal action in vitro. Moreover, the incorporation of iodine significantly decreased the minimal Nonoxynol-9 dose required for complete killing of spermatozoa in preparations containing Nonoxynol-9 oligomers 4 to 6 and 1 to 3. Conclusion(s) Incorporation of all three components tested in this study (PVP, Nonoxynol-9, and iodine) enhanced the efficiency of the spermicidal preparations, especially for Nonoxynol-9 preparations containing Nonoxynol-9 oligomers 4 to 6 and 1 to 3.

  • Solubilization and in Vitro Spermicidal Assessment of Nonoxynol-9 and Selected Fractions Using Rabbit Spermatozoa
    Pharmaceutical Research, 1991
    Co-Authors: Brian A. Walter, Amale A. Hawi, Panayiotis M Zavos, George A. Digenis
    Abstract:

    Selected oligomers representing the high, medium, and low molecular weight fractions of the spermicidal agent Nonoxynol-9 (N-9) were separated by HPLC. Nonoxynol-9 and the isolated fractions were formulated with polyvinylpyrrolidone (PVP) in order to increase their water solubility, particularly that of the insoluble low molecular weight fraction. The in vitro spermicidal activity of three molecular weight fractions were compared to that of N-9, using rabbit spermatozoa, at equimolar concentrations. Nonoxynol-9/PVP was far more effective in immobilizing the sperm than either N-9 alone or the separate fractions. The relative spermicidal activity of the oligomers was of the order middle molecular weight > high molecular weight > low molecular weight.

  • Solubilization and in vitro spermicidal assessment of Nonoxynol-9 and selected fractions using rabbit spermatozoa.
    Pharmaceutical research, 1991
    Co-Authors: Brian A. Walter, Amale A. Hawi, Panayiotis M Zavos, George A. Digenis
    Abstract:

    Selected oligomers representing the high, medium, and low molecular weight fractions of the spermicidal agent Nonoxynol-9 (N-9) were separated by HPLC. Nonoxynol-9 and the isolated fractions were formulated with polyvinylpyrrolidone (PVP) in order to increase their water solubility, particularly that of the insoluble low molecular weight fraction. The in vitro spermicidal activity of three molecular weight fractions were compared to that of N-9, using rabbit spermatozoa, at equimolar concentrations. Nonoxynol-9/PVP was far more effective in immobilizing the sperm than either N-9 alone or the separate fractions. The relative spermicidal activity of the oligomers was of the order middle molecular weight greater than high molecular weight greater than low molecular weight.

  • High-performance liquid chromatographic (HPLC) analysis of oligomeric components of the spermicide Nonoxynol-9.
    Pharmaceutical research, 1991
    Co-Authors: Brian A. Walter, George A. Digenis
    Abstract:

    The commercially available Nonoxynol-9 spermicide is a multicomponent mixture of oligomers. When Nonoxynol-9 was separated by normal phase gradient HPLC, 17 components were shown to exist in the commercial mixture. These oligomeric components follow a Poisson distribution around the most abundant oligomer, EO 8 (11.7%). Select oligomers were isolated by preparative HPLC (Rt = 19.6, 34.0, 45.6, 51.2, 61.6, and 79.2 min) and purified by HPLC. These were identified by FAB-MS and NMR to be the oligomers EO 3, EO 6, EO 8, EO 9, EO 11, and EO 16, respectively.

Sharon L. Hillier - One of the best experts on this subject based on the ideXlab platform.

  • Effects of long-term use of Nonoxynol-9 on vaginal flora
    Obstetrics and gynecology, 2006
    Co-Authors: Courtney A. Schreiber, Kurt T. Barnhart, Mitchell D. Creinin, Leslie A. Meyn, Sharon L. Hillier
    Abstract:

    Products containing Nonoxynol-9 have been used as spermicidal contraceptives for many years but limited data have been published describing the long-term effects of Nonoxynol-9 use on the vaginal microbial ecosystem. This longitudinal study was conducted to examine the effects of Nonoxynol-9 on the vaginal ecology. Vaginal swabs were obtained from 235 women enrolled in a randomized clinical trial before initiation of use of 1 of 5 different formulations of Nonoxynol-9 for contraception and up to 3 more samples were gathered over 7 months of use. The swab samples were evaluated in a single laboratory. The prevalence of several constituents of the normal vaginal flora was evaluated. The associations between Nonoxynol-9 dosage formulation average product use per week and number of sex acts per week were calculated. The changes in prevalence of vaginal microbes after Nonoxynol-9 use were minimal for each of the different Nonoxynol-9 formulations. However when both Nonoxynol-9 concentration and number of product uses are taken into account Nonoxynol-9 did have dose-dependant effects on the increased prevalence of anaerobic gram-negative rods (odds ratio [OR] 2.4 95% confidence interval [CI] 1.1-5.3) H/2O/2-negative lactobacilli (OR 2.0 95% CI 1.0-4.1) and bacterial vaginosis (OR 2.3 95% CI 1.1- 4.7). This study demonstrated that most Nonoxynol-9 users experienced minimal disruptions in their vaginal ecology. There were no differences between the different formulations evaluated with respect to changes in vaginal microflora. However independent of the Nonoxynol-9 formulation there was a dose-dependent effect with increased exposure to Nonoxynol-9 on the risk of bacterial vaginosis and its associated flora. (authors)

  • Why Nonoxynol-9 may have failed to prevent acquisition of Neisseria gonorrhoeae in clinical trials.
    Sexually transmitted diseases, 2005
    Co-Authors: Bernard J. Moncla, Sharon L. Hillier
    Abstract:

    Objectives: To understand why clinical trials failed to demonstrate efficacy of Nonoxynol-9 in preventing gonorrhea. Goal: To test the hypothesis that nonoyxnol-9 failed to prevent acquisition of Neisseria gonorrhoeae because most isolates are resistant to killing by nonoyxnol-9 at the level attainable with intravaginal use. Study: The lowest concentrations of Nonoxynol-9 required to kill or inhibit growth of clinical isolates of N gonorrhoeae and Lactobacillus were determined. Results: Most strains (17 of 25) of N gonorrhoeae (68%) were resistant to the highest concentration of Nonoxynol-9 tested (20%). L crispatus (100%), L jensenii (90%), and L iners (79%) were also resistant to Nonoxynol-9. Conclusions: N gonorrhoeae and H2O2-producing strains of vaginal lactobacilli were not killed by Nonoxynol-9 at concentrations greater than those achievable in vivo. Earlier studies that formed the basis for subsequent trials most likely did not detect resistance because too few isolates were evaluated. Large numbers of clinical isolates should be examined before the initiation of clinical trial using microbicidal products.

  • Effects of multiple applications of benzalkonium chloride and nonoxynol 9 on the vaginal epithelium in the pigtailed macaque (Macaca nemestrina)
    American journal of obstetrics and gynecology, 1999
    Co-Authors: Dorothy L. Patton, Gretchen Ganzle Kiddera, Yvonne Cosgrove Sweeneya, Lorna K. Rabeb, Sharon L. Hillier
    Abstract:

    Abstract Objective: Safe and effective vaginally applied microbicides could help to control the continuing spread of sexually transmitted diseases. Study Design: This study used nonhuman primates to test the effects of multiple applications of nonoxynol 9, benzalkonium chloride, or a combination on vaginal flora and lower reproductive tract tissues. Fourteen monkeys (Macaca nemestrina) received daily vaginal applications of nonoxynol 9, benzalkonium chloride, or both for 3 to 4 days. Vaginal microflora and colposcopic observations were made at baseline and during and after completion of treatments. Cervical biopsy specimens were collected from a subset of animals. Results: Cervical erythema and vaginal erythema were observed in all 3 treatment groups. Cervical papillae and epithelial disruption were present in both the nonoxynol 9 and the nonoxynol 9 plus benzalkonium chloride groups. Vaginal epithelial disruption was noted in both the benzalkonium chloride and the nonoxynol 9 plus benzalkonium chloride groups. Cervical biopsy specimens from each group revealed acute inflammatory infiltrates with occasional plasma cells and lymphoid follicles. Detection of most microorganisms, including viridans streptococci, decreased in the benzalkonium chloride and the nonoxynol 9 plus benzalkonium chloride groups. Detection of Lactobacillus species decreased in the benzalkonium chloride group. All microflora levels recovered after several days without microbicide use. Conclusions: Although nonoxynol 9 is currently the only microbicide approved for use as a spermicide in the United States, its repeated use may be detrimental to the epithelial tissues of the female reproductive tract. Benzalkonium chloride, currently approved for use in other countries, not only may damage epithelial tissues but also appears to reduce the population of potentially protective Lactobacillus species in the vagina. (Am J Obstet Gynecol 1999;180:1080-7.)

  • Effects of Nonoxynol-9 on vaginal microflora and chlamydial infection in a monkey model.
    Sexually transmitted diseases, 1996
    Co-Authors: Dorothy L. Patton, Gretchen Ganzle Kidder, Yvonne T. Cosgrove Sweeney, Lorna K. Rabe, Agnes M. Clark, Sharon L. Hillier
    Abstract:

    Background and Objectives: Nonoxynol-9, an intravaginal microbicide, is chlamydiacidal in vitro but also cytotoxic. This study examines the effects of Nonoxynol-9 in vivo, using a pigtail macaque model of chlamydial cervicitis. Goals: To establish a minimum infectious dose of Chlamydia trachomatis in the macaque, and to observe the effects of a single dose of Nonoxynol-9 on efficiency of chlamydial infection, vaginal microflora, and cervicovaginal irritation. Study Design: The effects of 4% Nonoxynol-9, C. trachomatis (5,000 or 10,000 IFU) or both Nonoxynol-9 application and chlamydial infection were studied in 17 macaques. Results: Following a single application of Nonoxynol-9, chlamydial infection was prevented in 4 of 6 monkeys infected with 10,000 IFU; there was a transient decrease in anaerobic gram-negative rods (P 0.05), but no change in Lactobacillus. Mild cervicovaginal irritation was observed in the monkeys. Conclusions: A single dose of Nonoxynol-9 causes minimal vaginal flora and epithelial irritation, and may be useful for prevention of chlamydial infection.

Andrew W. Bruce - One of the best experts on this subject based on the ideXlab platform.

  • The Influence of Nonoxynol-9-Containing Spermicides on Urogenital Infection
    The Journal of urology, 1994
    Co-Authors: Jacqueline A. Mcgroarty, Gregor Reid, Andrew W. Bruce
    Abstract:

    PIP: The most common spermicidal compound in use in North America is Nonoxynol-9. Barrier methods of contraception used in combination with a spermicidal product help prevent a variety of sexually transmitted diseases. In 1991 the Centers for Disease Control reported a total of 620,478 cases of gonorrhea, 128,569 of syphilis, and 43,672 of acquired immunodeficiency syndrome (AIDS). The evidence for antimicrobial activity of spermicides against sexually transmitted disease pathogens has been accumulated during the last 20 years from in vitro and in vivo studies on Neisseria gonorrhea, Treponema pallidum, Chlamydia trachomatis, Trichomonas vaginalis, Herpes simplex viruses 1 and 2, and the human immunodeficiency virus. Uropathogenic bacteria, including E. coli, Proteus mirabilis, Enterococcus faecalis and Staphylococcus species, have been found to grow in concentrations of 25% or greater of Nonoxynol-9. Less well known is the effect of Nonoxynol-9 on the growth of lactobacilli, the predominant organisms colonizing the vagina of most healthy postpubertal and premenopausal women, which according to in vitro studies could inhibit the colonization and ascending infection of the bladder by E. coli and as E. faecalis. The organisms associated with bacterial vaginosis have been found to be inhibited by low concentrations of Nonoxynol-9 (0.0019-0.5%). However, spermicide use does not appear to have any effect on the development of bacterial vaginosis. Clinical studies to date, with one exception, have shown no significant differences in bacterial vaginosis infection rates among users of diaphragms, contraceptive sponges and condoms and other contraceptive methods that do not involve exposure to spermicides. A history of Nonoxynol-9 use as well as the use of antimicrobial agents should be considered in recurrent urogenital infections, since both can potentially disrupt the urogenital microbial flora. The physician must weigh the risk of exposure to sexually transmitted diseases or an unwanted pregnancy against the prevention of urinary tract infection or vaginal candidiasis before advising the patient to discontinue the use of Nonoxynol-9-containing spermicides.

  • Hydrogen Peroxide Production by Lactobacillus Species: Correlation with Susceptibility to the Spermicidal Compound Nonoxynol-9
    The Journal of infectious diseases, 1992
    Co-Authors: Jacqueline A. Mcgroarty, Gregor Reid, Lisa Tomeczek, Donald G. Pond, Andrew W. Bruce
    Abstract:

    Facultative anaerobic lactobacilli were recovered from the vaginas of 96.8% of 63 nonpregnant, healthy, premenopausal women. The predominant species were Lactobacillus jensenii, Lactobacillus acidophilus, and Lactobacillus casei. Of the women, 74.6% had hydrogen peroxide-producing lactobacilli, 22.2% had non-hydrogen peroxide-producing lactobacilli, and 3.2% had no lactobacilli. None of the 68 isolates had catalase activity. Some 68.2% of the isolates were inhibited by concentrations of less than or equal to 1% (wt/vol) of Nonoxynol-9 (bactericidal for 73.3% of isolates, bacteriostatic for 26.7%). The remaining 31.8% could grow in all concentrations to 25% (wt/vol) of Nonoxynol-9. All of the lactobacilli that were sensitive to Nonoxynol-9 produced hydrogen peroxide whereas only 3 of 21 resistant strains were hydrogen peroxide producers. A significant correlation (P less than .001, chi 2 test) was found between hydrogen peroxide production and sensitivity to Nonoxynol-9. It is suggested that the vaginal flora of spermicide users could be depleted of hydrogen peroxide-producing lactobacilli, possibly increasing susceptibility to urogenital infection.

  • Correlation between hydrophobicity and resistance to nonoxynol‐9 and vancomycin for urogenital isolates of lactobacilli
    FEMS Microbiology Letters, 1992
    Co-Authors: Lisa Tomeczek, Jacqueline A. Mcgroarty, Gregor Reid, Andrew W. Bruce, Pieter L. Cuperus, Henny C. Van Der Mei, Antoine E. Khoury, Henk J. Busscher
    Abstract:

    Seven clinical isolates of lactobacilli were found to be relatively hydrophobic with a mean watercontact angle of 66 ± 15 degrees, and to be susceptible to 1% Nonoxynol-9 and vancomycin. However, seven other strains were relatively hydrophilic with a mean water-contact angle of 32 ± 13 degrees, and found to be resistant to 25% Nonoxynol-9 and vancomycin. Thus, the surface properties of lactobacilli that influence susceptibility to antimicrobial agents may involve surface hydrophobicity. Possibly the penetration barrier posed by the cell surface towards these two non-ionic antimicrobials is lower for hydrophobic cells than for hydrophilic cells.

Panayiotis M Zavos - One of the best experts on this subject based on the ideXlab platform.

  • Assessment of a tablet drug delivery system incorporating Nonoxynol-9 coprecipitated with polyvinylpyrrolidone in preventing the onset of pregnancy in rabbits
    Fertility and sterility, 1998
    Co-Authors: Panayiotis M Zavos, Juan R. Correa, Panayota N. Zarmakoupis-zavos
    Abstract:

    Abstract Objective: To assess the in vivo efficacy of the tablet drug delivery system containing Nonoxynol-9 coprecipitated with polyvinylpyrrolidone by delivering the spermicidal agents vaginally and evaluating their ability to prevent the onset of pregnancy in rabbits. Design: Controlled clinical study. Setting: Division of Laboratory and Animal Resources, College of Pharmacy, University of Kentucky. Animal(s): Forty-two New Zealand White female rabbits. Intervention(s): The rabbits were artificially inseminated at various intervals after vaginal insertion of the tablet drug delivery system containing either polyvinylpyrrolidone only (0 minutes) or Nonoxynol-9 coprecipitated with polyvinylpyrrolidone (polyvinylpyrrolidone/Nonoxynol-9; 0, 3, 30, 180, and 360 minutes). The rabbits were induced to ovulate 6 hours before insemination by IM injection of hCG (200 IU). Main Outcome Measure(s): The onset of pregnancy in the rabbits was evaluated after insertion of the tablet drug delivery system containing polyvinylpyrrolidone only or polyvinylpyrrolidone/Nonoxynol-9 at various intervals, followed by artificial insemination. Result(s): The onset of pregnancy was not reduced significantly when the tablet drug delivery system containing polyvinylpyrrolidone or polyvinylpyrrolidone/Nonoxynol-9 was used and insemination was performed immediately after tablet insertion (time 0). However, pregnancy rates (PRs) were reduced significantly in the rabbits that received the tablet drug delivery system containing polyvinylpyrrolidone/Nonoxynol-9 and were inseminated at 3, 30, 180, and 360 minutes after tablet insertion. The highest PR reduction occurred between 30 and 180 minutes after insertion of the tablet drug delivery system containing polyvinylpyrrolidone/Nonoxynol-9. Conclusion(s): The tablet drug delivery system is an efficient method of delivering the tested spermicidal agents vaginally. The design and dosage used in preparing the tablet drug delivery system provide short- and long-term release of the spermicidal agents, which results in almost immediate and extended enhancement of their contraceptive properties.

  • Assessment of new formulations of Nonoxynol-9 coprecipitated with polyvinylpyrrolidone and iodine as possible vaginal contraceptives
    Fertility and sterility, 1996
    Co-Authors: Panayiotis M Zavos, Juan R. Correa, Dagmar Nosek, Fatemeh Mohammadi, George A. Digenis
    Abstract:

    Objective To assess the in vitro spermicidal activity of new formulations of Nonoxynol-9, coprecipitated with polyvinylpyrrolidone (PVP) or iodinated PVP, against human spermatozoa via the use of the Sander-Cramer test and the cervical mucus penetration test. Design Solutions of PVP-Nonoxynol-9 and iodinated PVP-Nonoxynol-9 containing Nonoxynol-9 whole molecule (oligomers 1 to 18) and its isolated fractions (oligomers 8 to 10, 4 to 6, and 1 to 3) at various concentrations ( μ g/mL) were prepared via serial dilutions. Spermicidal solutions were mixed with human semen to determine the minimal lethal dose ( μ g/mL). In the Sander-Cramer test, the lethal dose was reported as the minimal dose capable of killing spermatozoa within 20 seconds. In the cervical mucus penetration test, the lethal dose was reported as the minimal dose capable of preventing penetration of spermatozoa into cervical mucus beyond the second millimeter length of the capillary. Setting Andrology laboratory, University of Kentucky, Lexington, Kentucky. Patient(s) Normospermic male donors. Main Outcome Measure(s) Spermicidal lethal dose determination of various Nonoxynol-9 preparations containing the whole Nonoxynol-9 molecule and its isolated fractions coprecipitated with PVP or iodinated PVP. Result(s) The use of PVP increased the aqueous solubility of the Nonoxynol-9 formulations containing oligomers 1 to 18 and 8 to 10 slightly. The coprecipitation of the Nonoxynol-9 formulations containing Nonoxynol-9 oligomers 4 to 6 and 1 to 3 with PVP significantly increased their solubilization and spermicidal action in vitro. Moreover, the incorporation of iodine significantly decreased the minimal Nonoxynol-9 dose required for complete killing of spermatozoa in preparations containing Nonoxynol-9 oligomers 4 to 6 and 1 to 3. Conclusion(s) Incorporation of all three components tested in this study (PVP, Nonoxynol-9, and iodine) enhanced the efficiency of the spermicidal preparations, especially for Nonoxynol-9 preparations containing Nonoxynol-9 oligomers 4 to 6 and 1 to 3.

  • Solubilization and in Vitro Spermicidal Assessment of Nonoxynol-9 and Selected Fractions Using Rabbit Spermatozoa
    Pharmaceutical Research, 1991
    Co-Authors: Brian A. Walter, Amale A. Hawi, Panayiotis M Zavos, George A. Digenis
    Abstract:

    Selected oligomers representing the high, medium, and low molecular weight fractions of the spermicidal agent Nonoxynol-9 (N-9) were separated by HPLC. Nonoxynol-9 and the isolated fractions were formulated with polyvinylpyrrolidone (PVP) in order to increase their water solubility, particularly that of the insoluble low molecular weight fraction. The in vitro spermicidal activity of three molecular weight fractions were compared to that of N-9, using rabbit spermatozoa, at equimolar concentrations. Nonoxynol-9/PVP was far more effective in immobilizing the sperm than either N-9 alone or the separate fractions. The relative spermicidal activity of the oligomers was of the order middle molecular weight > high molecular weight > low molecular weight.

  • Solubilization and in vitro spermicidal assessment of Nonoxynol-9 and selected fractions using rabbit spermatozoa.
    Pharmaceutical research, 1991
    Co-Authors: Brian A. Walter, Amale A. Hawi, Panayiotis M Zavos, George A. Digenis
    Abstract:

    Selected oligomers representing the high, medium, and low molecular weight fractions of the spermicidal agent Nonoxynol-9 (N-9) were separated by HPLC. Nonoxynol-9 and the isolated fractions were formulated with polyvinylpyrrolidone (PVP) in order to increase their water solubility, particularly that of the insoluble low molecular weight fraction. The in vitro spermicidal activity of three molecular weight fractions were compared to that of N-9, using rabbit spermatozoa, at equimolar concentrations. Nonoxynol-9/PVP was far more effective in immobilizing the sperm than either N-9 alone or the separate fractions. The relative spermicidal activity of the oligomers was of the order middle molecular weight greater than high molecular weight greater than low molecular weight.

Joseph A. Church - One of the best experts on this subject based on the ideXlab platform.

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