Renshall Lewis J, Beards Frances, Evangelinos Angelos, Greenwood Susan L, Brownbill Paul, Stevens Adam, Sibley Colin P, Aplin John D, Johnstone Edward D, Teesalu Tambet, Harris Lynda K
Maternal and Fetal Health Research Centre, Division of Developmental Biology and Medicine, Faculty of Biology, Medicine and Health, The University of Manchester, Manchester M13 9WL, UK.
Manchester Academic Health Science Centre, Central Manchester University Hospitals NHS Foundation Trust, St Mary's Hospital, Manchester M13 9WL, UK.
Pharmaceutics. 2021 Oct 25;13(11):1778. doi: 10.3390/pharmaceutics13111778.
Placental dysfunction is the underlying cause of pregnancy complications such as fetal growth restriction (FGR) and pre-eclampsia. No therapies are available to treat a poorly functioning placenta, primarily due to the risks of adverse side effects in both the mother and the fetus resulting from systemic drug delivery. The use of targeted liposomes to selectively deliver payloads to the placenta has the potential to overcome these issues. In this study, we assessed the safety and efficacy of epidermal growth factor (EGF)-loaded, peptide-decorated liposomes to improve different aspects of placental function, using tissue from healthy control pregnancies at term, and pregnancies complicated by FGR. Phage screening identified a peptide sequence, CGPSARAPC (GPS), which selectively homed to mouse placentas in vivo, and bound to the outer syncytiotrophoblast layer of human placental explants ex vivo. GPS-decorated liposomes were prepared containing PBS or EGF (50-100 ng/mL), and placental explants were cultured with liposomes for up to 48 h. Undecorated and GPS-decorated liposomes containing PBS did not affect the basal rate of amino acid transport, human chorionic gonadotropin (hCG) release or cell turnover in placental explants from healthy controls. GPS-decorated liposomes containing EGF significantly increased amino acid transporter activity in healthy control explants, but not in placental explants from women with FGR. hCG secretion and cell turnover were unaffected by EGF delivery; however, differential activation of downstream protein kinases was observed when EGF was delivered via GPS-decorated vs. undecorated liposomes. These data indicate that targeted liposomes represent a safe and useful tool for the development of new therapies for placental dysfunction, recapitulating the effects of free EGF.
胎盘功能障碍是胎儿生长受限(FGR)和先兆子痫等妊娠并发症的根本原因。目前尚无治疗胎盘功能不良的疗法,主要是因为全身给药会给母体和胎儿带来不良副作用风险。使用靶向脂质体将药物选择性地递送至胎盘有可能克服这些问题。在本研究中,我们使用足月健康对照妊娠组织和合并FGR的妊娠组织,评估了负载表皮生长因子(EGF)、经肽修饰的脂质体改善胎盘功能不同方面的安全性和有效性。噬菌体筛选确定了一个肽序列CGPSARAPC(GPS),该序列在体内可选择性归巢至小鼠胎盘,并在体外与人胎盘外植体的外合体滋养层结合。制备了含有PBS或EGF(50 - 100 ng/mL)的经GPS修饰的脂质体,并将胎盘外植体与脂质体一起培养长达48小时。未修饰的和含有PBS的经GPS修饰的脂质体对健康对照胎盘外植体的氨基酸转运基础速率、人绒毛膜促性腺激素(hCG)释放或细胞更新没有影响。含有EGF的经GPS修饰的脂质体显著增加了健康对照外植体中的氨基酸转运蛋白活性,但对FGR女性的胎盘外植体没有影响。EGF递送不影响hCG分泌和细胞更新;然而,当通过经GPS修饰的脂质体与未修饰的脂质体递送EGF时,观察到下游蛋白激酶的不同激活。这些数据表明,靶向脂质体是开发胎盘功能障碍新疗法的安全且有用的工具,可重现游离EGF的作用。