载有地高辛的聚合物纳米颗粒通过BeWo细胞（人胎盘滋养层细胞的体外模型）的转运。
Transport of digoxin-loaded polymeric nanoparticles across BeWo cells, an in vitro model of human placental trophoblast.
作者信息
Albekairi Norah A, Al-Enazy Sanaalarab, Ali Shariq, Rytting Erik
机构信息
Department of Pharmacology & Toxicology, University of Texas Medical Branch, Galveston, TX 77555, USA.
Department of Obstetrics & Gynecology, University of Texas Medical Branch, Galveston, TX 77555, USA.
出版信息
Ther Deliv. 2015;6(12):1325-34. doi: 10.4155/tde.15.79.
BACKGROUND
Fetal arrhythmias can lead to fetal congestive heart failure and hydrops fetalis. Digoxin (the first-line treatment) has low transplacental permeability and high risk of maternal side effects. Biodegradable digoxin-loaded PEGylated poly(lactic-co-glycolic acid) nanoparticles may increase digoxin transport across BeWo b30 cell monolayers (an in vitro model of trophoblast in human placenta) by reducing the drug's interaction with P-gp. Results/methodology: The nanoparticles showed high encapsulation efficiency and sustained release over 48 h. Transport studies revealed significantly increased permeability across BeWo cell layers of digoxin-loaded nanoparticles when compared with free digoxin. P-gp inhibition also increased the permeability of digoxin, but not digoxin-loaded nanoparticles.
CONCLUSION
This represents a novel treatment strategy for fetal cardiovascular disease which may improve maternal and fetal outcomes.
背景
胎儿心律失常可导致胎儿充血性心力衰竭和胎儿水肿。地高辛（一线治疗药物）经胎盘的通透性低，且母体副作用风险高。可生物降解的载地高辛聚乙二醇化聚乳酸-羟基乙酸纳米粒可能通过减少药物与P-糖蛋白的相互作用，增加地高辛穿过BeWo b30细胞单层（人胎盘滋养层细胞的体外模型）的转运。结果/方法：纳米粒显示出高包封率，并在48小时内持续释放。转运研究表明，与游离地高辛相比，载地高辛纳米粒穿过BeWo细胞层的通透性显著增加。P-糖蛋白抑制也增加了地高辛的通透性，但对载地高辛纳米粒没有影响。
结论
这代表了一种治疗胎儿心血管疾病的新策略，可能改善母体和胎儿的结局。
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