Transdermal delivery of antenatal steroids to promote fetal lung maturation: Proof of principle data from sheep and non-human primate models

Abstract Background Antenatal steroids (ANS) are routinely administered to women at risk of preterm birth to accelerate fetal lung maturation. Despite extensive clinical use, dosing and route of ANS administration remain unoptimized beyond intramuscular (IM) injection. We aimed to undertake a proof-...

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Main Authors: Sean W. D. Carter, Ayça Altay Benetti, Ryan Tze Liang Sia, Giorgia Pastorin, Erin L. Johnson, Kay Yi Michelle Seah, Haruo Usuda, Hannah R. S. Watson, Yusaku Kumagai, Qin Wei, Xiawen Liu, Roberto Orefice, Marianne Bon, Zubair Amin, Agnihotri Biswas, Tsukasa Takahashi, Noriyoshi Mochii, Yuya Saito, Hideyuki Ikeda, Masatoshi Saito, Mahesh A. Choolani, Sebastián E. Illanes, Matthew W. Kemp
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Language:English
Published: BMC 2025-08-01
Series:BMC Medicine
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Online Access:https://doi.org/10.1186/s12916-025-04267-9
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author Sean W. D. Carter
Ayça Altay Benetti
Ryan Tze Liang Sia
Giorgia Pastorin
Erin L. Johnson
Kay Yi Michelle Seah
Haruo Usuda
Hannah R. S. Watson
Yusaku Kumagai
Qin Wei
Xiawen Liu
Roberto Orefice
Marianne Bon
Zubair Amin
Agnihotri Biswas
Tsukasa Takahashi
Noriyoshi Mochii
Yuya Saito
Hideyuki Ikeda
Masatoshi Saito
Mahesh A. Choolani
Sebastián E. Illanes
Matthew W. Kemp
author_facet Sean W. D. Carter
Ayça Altay Benetti
Ryan Tze Liang Sia
Giorgia Pastorin
Erin L. Johnson
Kay Yi Michelle Seah
Haruo Usuda
Hannah R. S. Watson
Yusaku Kumagai
Qin Wei
Xiawen Liu
Roberto Orefice
Marianne Bon
Zubair Amin
Agnihotri Biswas
Tsukasa Takahashi
Noriyoshi Mochii
Yuya Saito
Hideyuki Ikeda
Masatoshi Saito
Mahesh A. Choolani
Sebastián E. Illanes
Matthew W. Kemp
author_sort Sean W. D. Carter
collection DOAJ
description Abstract Background Antenatal steroids (ANS) are routinely administered to women at risk of preterm birth to accelerate fetal lung maturation. Despite extensive clinical use, dosing and route of ANS administration remain unoptimized beyond intramuscular (IM) injection. We aimed to undertake a proof-of-principle assessment of transdermal ANS administration for accelerated fetal lung maturation. Methods We formulated and tested a transdermal ANS (betamethasone) patch in ex vivo studies. To confirm in vivo transdermal distribution of the ANS patch, we undertook a 24-h pharmacokinetic study in non-pregnant cynomolgus macaques (NHP). To assess the efficacy of transdermal betamethasone on fetal lung maturation, we used a preterm sheep model of pregnancy comparing postnatal ventilation outcomes. Date mated ewes received either of the following: (i) IM normal saline (Saline Control, n = 13); (ii) IM ANS (betamethasone) delivery 2 or 8 days post-treatment (2-Day IM ANS, n = 14; 8-day IM ANS Group, n = 6); (iii) IM saline + 2 × transdermal ANS (Betamethasone) patches delivery 2 days post-treatment (2-Day ANS Patch, n = 10); or (iv) IM saline + 2 × transdermal ANS (betamethasone) patches replaced with 2 × new patches after 48 h, delivery 8 days post-treatment (8-Day ANS Patch, n = 11). Lambs were delivered at 123 ± 1 dGA (term 150 days), then ventilated for 30 min to assess lung maturation status. Arterial blood gas, delivery, and ventilation data were analyzed (p < 0.05 significant). Results Transdermal administration of ANS in NHPs achieved rapid plasma accumulation, with a plasma half-life of 8.9 h, similar to that achieved with IM dosing in clinical practice. In preterm sheep, all 2- and 8-day IM and transdermal ANS patch groups had clinically important and statistically significant improvements in ventilation parameters (umbilical PaCO2, pH, tidal volume) compared to saline control. Conclusions We demonstrate, for the first time, the potential for using transdermal ANS for preterm fetal lung maturation. Transdermal ANS administration eliminates the need for injections, pain, and infection risk. Moreover, transdermal ANS delivery demonstrates advantages in dose control, continuity of exposure, and potential to remove drug exposure should the risk of preterm birth resolve. Further development of this technology may improve preterm outcomes through delivery of a low dose, constant fetal steroid exposure.
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spelling doaj-art-8e0a0598142f45ef8b2d44e35ac815702025-08-20T03:46:07ZengBMCBMC Medicine1741-70152025-08-0123111510.1186/s12916-025-04267-9Transdermal delivery of antenatal steroids to promote fetal lung maturation: Proof of principle data from sheep and non-human primate modelsSean W. D. Carter0Ayça Altay Benetti1Ryan Tze Liang Sia2Giorgia Pastorin3Erin L. Johnson4Kay Yi Michelle Seah5Haruo Usuda6Hannah R. S. Watson7Yusaku Kumagai8Qin Wei9Xiawen Liu10Roberto Orefice11Marianne Bon12Zubair Amin13Agnihotri Biswas14Tsukasa Takahashi15Noriyoshi Mochii16Yuya Saito17Hideyuki Ikeda18Masatoshi Saito19Mahesh A. Choolani20Sebastián E. Illanes21Matthew W. Kemp22Department of Obstetrics and Gynaecology, Yong Loo Lin School of Medicine, National University of SingaporeDepartment of Pharmacy and Pharmaceutical Sciences, National University of SingaporeDepartment of Pharmacy and Pharmaceutical Sciences, National University of SingaporeDepartment of Pharmacy and Pharmaceutical Sciences, National University of SingaporeDivision of Obstetrics and Gynaecology, University of Western AustraliaDepartment of Obstetrics and Gynaecology, Yong Loo Lin School of Medicine, National University of SingaporeDivision of Obstetrics and Gynaecology, University of Western AustraliaDivision of Obstetrics and Gynaecology, University of Western AustraliaDepartment of Obstetrics and Gynaecology, Yong Loo Lin School of Medicine, National University of SingaporeDepartment of Obstetrics and Gynaecology, Yong Loo Lin School of Medicine, National University of SingaporeDepartment of Obstetrics and Gynaecology, Yong Loo Lin School of Medicine, National University of SingaporeSchool of Medicine and Psychology, Australian National UniversityKing Edward Memorial HospitalDepartment of Neonatology, Khoo-Teck Puat National University Children’s Medical Institute, National University HospitalDepartment of Neonatology, Khoo-Teck Puat National University Children’s Medical Institute, National University HospitalCentre for Perinatal and Neonatal Medicine, Tohoku University HospitalCentre for Perinatal and Neonatal Medicine, Tohoku University HospitalCentre for Perinatal and Neonatal Medicine, Tohoku University HospitalDivision of Obstetrics and Gynaecology, University of Western AustraliaCentre for Perinatal and Neonatal Medicine, Tohoku University HospitalDepartment of Obstetrics and Gynaecology, Yong Loo Lin School of Medicine, National University of SingaporeDepartment of Obstetrics and Gynaecology, Yong Loo Lin School of Medicine, National University of SingaporeDepartment of Obstetrics and Gynaecology, Yong Loo Lin School of Medicine, National University of SingaporeAbstract Background Antenatal steroids (ANS) are routinely administered to women at risk of preterm birth to accelerate fetal lung maturation. Despite extensive clinical use, dosing and route of ANS administration remain unoptimized beyond intramuscular (IM) injection. We aimed to undertake a proof-of-principle assessment of transdermal ANS administration for accelerated fetal lung maturation. Methods We formulated and tested a transdermal ANS (betamethasone) patch in ex vivo studies. To confirm in vivo transdermal distribution of the ANS patch, we undertook a 24-h pharmacokinetic study in non-pregnant cynomolgus macaques (NHP). To assess the efficacy of transdermal betamethasone on fetal lung maturation, we used a preterm sheep model of pregnancy comparing postnatal ventilation outcomes. Date mated ewes received either of the following: (i) IM normal saline (Saline Control, n = 13); (ii) IM ANS (betamethasone) delivery 2 or 8 days post-treatment (2-Day IM ANS, n = 14; 8-day IM ANS Group, n = 6); (iii) IM saline + 2 × transdermal ANS (Betamethasone) patches delivery 2 days post-treatment (2-Day ANS Patch, n = 10); or (iv) IM saline + 2 × transdermal ANS (betamethasone) patches replaced with 2 × new patches after 48 h, delivery 8 days post-treatment (8-Day ANS Patch, n = 11). Lambs were delivered at 123 ± 1 dGA (term 150 days), then ventilated for 30 min to assess lung maturation status. Arterial blood gas, delivery, and ventilation data were analyzed (p < 0.05 significant). Results Transdermal administration of ANS in NHPs achieved rapid plasma accumulation, with a plasma half-life of 8.9 h, similar to that achieved with IM dosing in clinical practice. In preterm sheep, all 2- and 8-day IM and transdermal ANS patch groups had clinically important and statistically significant improvements in ventilation parameters (umbilical PaCO2, pH, tidal volume) compared to saline control. Conclusions We demonstrate, for the first time, the potential for using transdermal ANS for preterm fetal lung maturation. Transdermal ANS administration eliminates the need for injections, pain, and infection risk. Moreover, transdermal ANS delivery demonstrates advantages in dose control, continuity of exposure, and potential to remove drug exposure should the risk of preterm birth resolve. Further development of this technology may improve preterm outcomes through delivery of a low dose, constant fetal steroid exposure.https://doi.org/10.1186/s12916-025-04267-9Antenatal corticosteroidsPreterm birthTransdermal patchOptimizing route of administrationFetal lung maturationPerinatal medicine
spellingShingle Sean W. D. Carter
Ayça Altay Benetti
Ryan Tze Liang Sia
Giorgia Pastorin
Erin L. Johnson
Kay Yi Michelle Seah
Haruo Usuda
Hannah R. S. Watson
Yusaku Kumagai
Qin Wei
Xiawen Liu
Roberto Orefice
Marianne Bon
Zubair Amin
Agnihotri Biswas
Tsukasa Takahashi
Noriyoshi Mochii
Yuya Saito
Hideyuki Ikeda
Masatoshi Saito
Mahesh A. Choolani
Sebastián E. Illanes
Matthew W. Kemp
Transdermal delivery of antenatal steroids to promote fetal lung maturation: Proof of principle data from sheep and non-human primate models
BMC Medicine
Antenatal corticosteroids
Preterm birth
Transdermal patch
Optimizing route of administration
Fetal lung maturation
Perinatal medicine
title Transdermal delivery of antenatal steroids to promote fetal lung maturation: Proof of principle data from sheep and non-human primate models
title_full Transdermal delivery of antenatal steroids to promote fetal lung maturation: Proof of principle data from sheep and non-human primate models
title_fullStr Transdermal delivery of antenatal steroids to promote fetal lung maturation: Proof of principle data from sheep and non-human primate models
title_full_unstemmed Transdermal delivery of antenatal steroids to promote fetal lung maturation: Proof of principle data from sheep and non-human primate models
title_short Transdermal delivery of antenatal steroids to promote fetal lung maturation: Proof of principle data from sheep and non-human primate models
title_sort transdermal delivery of antenatal steroids to promote fetal lung maturation proof of principle data from sheep and non human primate models
topic Antenatal corticosteroids
Preterm birth
Transdermal patch
Optimizing route of administration
Fetal lung maturation
Perinatal medicine
url https://doi.org/10.1186/s12916-025-04267-9
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