Effect of a novel contraceptive compound on vaginal health
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In 2011, 49 percent of pregnancies in the United States were unintended. There are currently available over the counter contraceptive options, such as condoms and spermicides, but these methods have failure rates between 13-21 percent. Additionally, spermicides can cause damage to the vaginal epithelium and can increase susceptibility to sexually transmitted diseases (STDs). As such, our laboratory has identified a novel non-hormonal contraceptive method to block the semen liquefaction process using a small molecule inhibitor called triazole B1. B1 acts to block the activity of prostate specific antigen, the serine protease responsible for initiating the liquefaction process by cleaving the protein SEMG-1. B1 is intended to be used as a local vaginal gel contraceptive and not as a systemic drug. Therefore, we need to address whether B1 can penetrate the vaginal epithelial layer. Using human liver microsomes (HLM), we found that B1 is not fully metabolized by liver microsomes and is detectable by UHPLC- MS in its original form. To determine if B1 can traverse the vaginal epithelium and enter circulation, we preformed tissue permeation experiments using Mattek's 3D human EpiVaginal tissue. B1 was not able to traverse human vaginal ectocervical cells in vitro. Next, we tested B1's permeability in a murine in vivo model, again finding that B1 was not able to permeate the vaginal epithelial layer. Together, these findings suggest that B1 will remain within the vagina and not reach systemic circulation.
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M.S.