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A thermosensitive gel based on w1/o/w2 multiple microemulsions for the vaginal delivery of small nucleic acid

The present study aims at designing a thermosensitive gel prepared from w1/o/w2 multiple microemulsions (MMEs) for the vaginal delivery of siRNA. The w1/o/w2 MMEs were prepared by two-step emulsifications: the first step was to prepare primary emulsions (w1/o) by low energy emulsification (LEE); the...

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Autores principales: Wang, Jiu, Wang, Yajing, Wang, Ziqiang, Wang, Fan, He, Jie, Yang, Xiaoyun, Xie, Weidong, Liu, Ying, Zhang, Yaou
Formato: Online Artículo Texto
Lenguaje:English
Publicado: Taylor & Francis 2019
Materias:
Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC6407577/
https://www.ncbi.nlm.nih.gov/pubmed/30822166
http://dx.doi.org/10.1080/10717544.2019.1568622
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author Wang, Jiu
Wang, Yajing
Wang, Ziqiang
Wang, Fan
He, Jie
Yang, Xiaoyun
Xie, Weidong
Liu, Ying
Zhang, Yaou
author_facet Wang, Jiu
Wang, Yajing
Wang, Ziqiang
Wang, Fan
He, Jie
Yang, Xiaoyun
Xie, Weidong
Liu, Ying
Zhang, Yaou
author_sort Wang, Jiu
collection PubMed
description The present study aims at designing a thermosensitive gel prepared from w1/o/w2 multiple microemulsions (MMEs) for the vaginal delivery of siRNA. The w1/o/w2 MMEs were prepared by two-step emulsifications: the first step was to prepare primary emulsions (w1/o) by low energy emulsification (LEE); the second step was to obtain stable w1/o/w2 MMEs by self-emulsifying. An extensive formulation optimization process was undertaken. The final w1/o/w2 MMEs could be formed in ddH(2)O, phosphate buffer solution (PBS, pH 7.4) and 1640 culture media with diameter size about 166.5 ± 13.1, 271.0 ± 11.1 and 278.7 ± 12.1 nm respectively. The release rates of siRNA from solutions, MMEs and MMEs-gels were completed within 2 h, 6 h and13 h respectively. The transfection efficiency of MMEs was confirmed both in vitro and in vivo. The relative target gene expressions of MMEs were 0.07 ± 0.05% vs. 0.37 ± 0.06% in Hela cells against Lipofectamine2000® and 1.88% ± 0.00% vs. 9.65% ± 0.02% in mouse vaginal mucosa against PEI. Good biocompatibility of MMEs was verified by cytotoxicity and pathological studies. Overall, our results indicated the potential of the MMEs-gel system for the vaginal delivery of siRNA.
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spelling pubmed-64075772019-03-12 A thermosensitive gel based on w1/o/w2 multiple microemulsions for the vaginal delivery of small nucleic acid Wang, Jiu Wang, Yajing Wang, Ziqiang Wang, Fan He, Jie Yang, Xiaoyun Xie, Weidong Liu, Ying Zhang, Yaou Drug Deliv Research Article The present study aims at designing a thermosensitive gel prepared from w1/o/w2 multiple microemulsions (MMEs) for the vaginal delivery of siRNA. The w1/o/w2 MMEs were prepared by two-step emulsifications: the first step was to prepare primary emulsions (w1/o) by low energy emulsification (LEE); the second step was to obtain stable w1/o/w2 MMEs by self-emulsifying. An extensive formulation optimization process was undertaken. The final w1/o/w2 MMEs could be formed in ddH(2)O, phosphate buffer solution (PBS, pH 7.4) and 1640 culture media with diameter size about 166.5 ± 13.1, 271.0 ± 11.1 and 278.7 ± 12.1 nm respectively. The release rates of siRNA from solutions, MMEs and MMEs-gels were completed within 2 h, 6 h and13 h respectively. The transfection efficiency of MMEs was confirmed both in vitro and in vivo. The relative target gene expressions of MMEs were 0.07 ± 0.05% vs. 0.37 ± 0.06% in Hela cells against Lipofectamine2000® and 1.88% ± 0.00% vs. 9.65% ± 0.02% in mouse vaginal mucosa against PEI. Good biocompatibility of MMEs was verified by cytotoxicity and pathological studies. Overall, our results indicated the potential of the MMEs-gel system for the vaginal delivery of siRNA. Taylor & Francis 2019-03-01 /pmc/articles/PMC6407577/ /pubmed/30822166 http://dx.doi.org/10.1080/10717544.2019.1568622 Text en © 2019 The Author(s). Published by Informa UK Limited, trading as Taylor & Francis Group. http://creativecommons.org/licenses/by/4.0/ This is an Open Access article distributed under the terms of the Creative Commons Attribution License (http://creativecommons.org/licenses/by/4.0/), which permits unrestricted use, distribution, and reproduction in any medium, provided the original work is properly cited.
spellingShingle Research Article
Wang, Jiu
Wang, Yajing
Wang, Ziqiang
Wang, Fan
He, Jie
Yang, Xiaoyun
Xie, Weidong
Liu, Ying
Zhang, Yaou
A thermosensitive gel based on w1/o/w2 multiple microemulsions for the vaginal delivery of small nucleic acid
title A thermosensitive gel based on w1/o/w2 multiple microemulsions for the vaginal delivery of small nucleic acid
title_full A thermosensitive gel based on w1/o/w2 multiple microemulsions for the vaginal delivery of small nucleic acid
title_fullStr A thermosensitive gel based on w1/o/w2 multiple microemulsions for the vaginal delivery of small nucleic acid
title_full_unstemmed A thermosensitive gel based on w1/o/w2 multiple microemulsions for the vaginal delivery of small nucleic acid
title_short A thermosensitive gel based on w1/o/w2 multiple microemulsions for the vaginal delivery of small nucleic acid
title_sort thermosensitive gel based on w1/o/w2 multiple microemulsions for the vaginal delivery of small nucleic acid
topic Research Article
url https://www.ncbi.nlm.nih.gov/pmc/articles/PMC6407577/
https://www.ncbi.nlm.nih.gov/pubmed/30822166
http://dx.doi.org/10.1080/10717544.2019.1568622
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