首批用于可逆性非荷尔蒙男性避孕的皮下注射.
Sarah Anne Howard1, James K Tsuruta2, Andres Prieto Trujillo1
1Division of Pharmacoengineering and Molecular Pharmaceutics, UNC Eshelman School of Pharmacy, University of North Carolina at Chapel Hill, Chapel Hill, NC, USA.
研究人员开发了一种新的可注射男性避孕药,使用在现场形成植入物 (ISFI) 中的EP055. 这种非荷尔蒙选择显示了可逆的避孕效应,并且在小鼠中耐受良好,支持未来男性避孕药的发展.
科学领域:
- 生殖生物学 生殖生物学
- 药理学 药理学是指药理学的学科.
- 生物材料科学是生物材料的科学.
背景情况:
- 目前男性避孕方法仅限于避孕套和输精管切除术.
- 需要可逆,高效的男性避孕方案.
- EP055是一种具有潜在避孕作用的新型非激素化合物.
研究的目的:
- 将EP055配制成一种在位形成植入物 (ISFI),用于长效可注射的男性避孕.
- 评估EP055-ISFI在雄性小鼠中的安全性,药理动力学和疗效.
主要方法:
- 开发和优化了EP055-ISFI配方. 开发和优化了EP055-ISFI配方.
- 在35天内研究了体外释放动力学.
- 对雄性BALB/c小鼠进行了体内研究,以评估安全性,PK和疗效.
主要成果:
- 优化EP055-ISFI (F.04) 在试验室中显示持续释放.
- 在体内研究表明EP055 ISFI引起的爆发释放,随后持续的血度高达28天.
- EP055 ISFI的使用降低了精子的运动性和增加了过早的体膜降解,表明了避孕疗法的有效性.
- 该化合物耐受性良好,没有系统性炎症.
结论:
- EP055-ISFI是一种有前途的长效注射男性避孕药.
- 该配方在小鼠中表现出可逆的避孕效果和良好的安全性.
- 结果支持进一步开发用于男性避孕的EPPIN向分子和ISFI.
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