Population Council, 1230 York Avenue, New York, NY, 10065, USA.
Aaron Diamond AIDS Research Center, 455 First Avenue, 7th Floor, New York, NY, 10016, USA.
Drug Deliv Transl Res. 2017 Dec;7(6):840-858. doi: 10.1007/s13346-017-0389-0.
Women globally need access to multipurpose prevention technologies (MPTs) that prevent human immunodeficiency virus (HIV), sexually transmitted infections that increase HIV acquisition/transmission risk, and unintended pregnancy. Seeking an MPT with activity against HIV, herpes simplex virus-2 (HSV-2), and human papillomavirus (HPV), we developed a prototype intravaginal ring (IVR), the MZCL IVR, which released the antiviral agents MIV-150, zinc acetate, and carrageenan (MZC for short) and the contraceptive levonorgestrel (LNG). Previously, we showed that an MZC gel has potent activity against immunodeficiency viruses, HSV-2, and HPV and that the MZCL (MZC with LNG) IVR releases all four components in macaques in vivo at levels associated with efficacy. Vaginal fluid from treated macaques has in vitro activity against HIV, HSV-2, and HPV. Herein, we assessed the ability of the MZCL IVR to protect macaques against repeated co-challenge with HSV-2 and SHIV-RT (simian immunodeficiency virus [SIV] containing the reverse transcriptase gene from HIV) and prevent hormonal cycling. We evaluated in vivo drug release in co-challenged macaques by measuring drug levels in blood and vaginal fluid and residual drug levels in used IVRs. The MZCL IVR significantly prevented SHIV-RT infection, reduced HSV-2 vaginal shedding, and prevented cycling. No non-nucleoside HIV reverse transcriptase inhibitor (NNRTI)-resistant SHIV was detected in macaques that became infected after continuous exposure to MZC from the IVR. Macaques wearing the MZCL IVR also had carrageenan levels in vaginal fluid expected to protect from HPV (extrapolated from mice) and LNG levels in blood associated with contraceptive efficacy. The MZCL IVR is a promising MPT candidate that warrants further development.
全球女性都需要获得多用途预防技术(MPT),这些技术可以预防人类免疫缺陷病毒(HIV)、增加 HIV 获得/传播风险的性传播感染以及意外怀孕。为了寻找一种对 HIV、单纯疱疹病毒-2(HSV-2)和人乳头瘤病毒(HPV)都有活性的 MPT,我们开发了一种原型阴道环(IVR),即 MZCL IVR,它释放抗病毒药物 MIV-150、醋酸锌和角叉菜胶(简称 MZC)和避孕药左炔诺孕酮(LNG)。此前,我们表明 MZC 凝胶对免疫缺陷病毒、HSV-2 和 HPV 具有强大的活性,并且 MZCL(含 LNG 的 MZC)IVR 在体内释放所有四种成分,其水平与疗效相关。接受治疗的猕猴阴道液具有体外抗 HIV、HSV-2 和 HPV 的活性。在此,我们评估了 MZCL IVR 保护猕猴免受 HSV-2 和 SHIV-RT(含有 HIV 逆转录酶基因的猴免疫缺陷病毒 [SIV])重复共挑战以及防止激素循环的能力。我们通过测量血液和阴道液中的药物水平以及使用过的 IVR 中的残留药物水平来评估共挑战猕猴中的体内药物释放。MZCL IVR 显著预防了 SHIV-RT 感染,减少了 HSV-2 阴道脱落,并防止了循环。在持续暴露于 IVR 中的 MZC 后,连续接触仍感染的猕猴中未检测到非核苷类 HIV 逆转录酶抑制剂(NNRTI)耐药性 SHIV。佩戴 MZCL IVR 的猕猴阴道液中的角叉菜胶水平也有望预防 HPV(从老鼠推断),而血液中的 LNG 水平与避孕效果相关。MZCL IVR 是一种很有前途的 MPT 候选物,值得进一步开发。