Spermicidal agents Benzalkonium chloride and Nonoxynol-9: In vitro comparative efficacy and tolerance
ESC Congress Library. Tavares R. May 10, 2018; 208061; ESC8
Dr. Renata S. Tavares
Dr. Renata S. Tavares
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Abstract
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Introduction/objectives: Acrosomal integrity and motility are essential for the fertilizing ability of spermatozoa; they should be strongly affected by spermicidal vaginal formulations in order to prevent undesirable pregnancies. Benzalkonium chloride (BZK) and Nonoxynol-9 (N9) are two active principles with surfactant properties that have been used for more than 30 years in such formulations. However, despite their wide clinical use, there are few comparative reports on their efficacy and local tolerance. Thus the goals of this study were to compare 1) the efficacy and 2) the tolerance of BZK and N9 in vitro using human sperm samples and a cervical/vaginal cell line. Design and Methods: For the comparative efficacy, commercialized formulations containing 18.9 mg BZK (Pharmatex® mini-pessaries) or 75.0 mg N9 (Patentex® oval N) were tested. Normozoospermic samples were exposed to either an untreated control or both formulations for 0 or 20 minutes after dilution in a specific volume of medium deemed to reflect the in vivo vaginal/cervical conditions. The acrosomal status was determined using the specific acrosomal marker PSA-FITC, while sperm motility was evaluated by simple phase-contrast microscopy and by the Sander-Cramer test. Sperm viability was assessed by the eosin exclusion test.                                                                                                                                                   For the comparative tolerance assessment, the active pharmaceutical ingredients were tested. HeLa cells were exposed for 0, 1 hour or 2 hours to either an untreated control, 18.9 mg BZK or 75.0 mg N9 diluted as above. Their viability was monitored by the colorimetric MTT assay that assesses metabolic activity. Results: Upon immediate contact and after 20 minutes of exposure, BZK formulation promoted a severe loss of acrosome integrity (98.8%/99.95%) by comparison with N9 formulation (75.1%/89.5% - p From the beginning of exposure both BZK and N9 negatively affected HeLa cells viability by comparison with the untreated control. However, this effect was even more drastic with N9 when compared to BZK from time 0 and onwards. In addition, unlike BZK, N9 was responsible for cell detachment - a clear sign of cell death. Conclusions: Under the conditions of these in vitro tests, BZK has shown a more efficient spermicidal activity than N9 by inducing a more severe acrosome loss, while being better tolerated by HeLa cells. Funding: This study is supported by laboratoire INNOTECH International S.A.S.
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