Comparative <i>in vitro</i> study on the local tolerance and efficacy of benzalkonium chloride, myristalkonium chloride and nonoxynol-9 as active principles in vaginal contraceptives

Spermicides have been identified as a potentially attractive alternative to hormonal contraceptives and/or intrauterine devices. Thus, this study aimed evaluating the efficacy and local tolerance of benzalkonium chloride (BKC) and myristalkonium chloride (MKC) contained in Pharmatex^® vaginal formulations and compare them with nonoxynol-9 (N-9), the most common active ingredient in topical vaginal contraceptives. Human normozoospermic samples were assessed for motility, viability, acrosome status and penetration ability after exposure to control, N-9 or different BKC and MKC doses for 0 and 10 minutes. Local tolerance on HeLa cells was evaluated by the Trypan-blue and MTT assays. Exposure to BKC and MKC reduced acrosome integrity while promoting total immobilisation and complete loss of sperm viability (<i>p</i> n = 15). Both compounds also compromised sperm penetration ability upon exposure (<i>p</i> n = 15). N-9 induced the same outcomes (<i>p</i> n = 15); nevertheless, it was more toxic to HeLa cells than BKC and MKC (<i>p</i> n = 14). BKC and MKC present strong <i>in vitro</i> spermicidal activity at lower doses than N-9 and were better tolerated after immediate exposure than N-9. Available Pharmatex^® galenic formulations were as effective as products based on N-9.