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Oil–water partition coefficient preparation and detection in the dihydroartemisinin self-emulsifying drug delivery system

BACKGROUND: The aim of the present study is to increase the solubility of dihydroartemisinin (DHA) using the self-emulsifying drug delivery system (SEDDS). METHODS: We first conducted solubility test and ternary phase diagram, then, in order to optimize the formulation of the DHA self-emulsifying ag...

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Autores principales: Wang, Yunhong, Chen, Jingcai, Yang, Yang, Gao, Sijia, Wang, Zhuzhu, Liu, Yating, Zhang, Xiaomei, Hua, Lei, Guo, Yanlei, Yang, Yong
Formato: Online Artículo Texto
Lenguaje:English
Publicado: BioMed Central 2022
Materias:
Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC9137071/
https://www.ncbi.nlm.nih.gov/pubmed/35624465
http://dx.doi.org/10.1186/s12896-022-00746-6
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author Wang, Yunhong
Chen, Jingcai
Yang, Yang
Gao, Sijia
Wang, Zhuzhu
Liu, Yating
Zhang, Xiaomei
Hua, Lei
Guo, Yanlei
Yang, Yong
author_facet Wang, Yunhong
Chen, Jingcai
Yang, Yang
Gao, Sijia
Wang, Zhuzhu
Liu, Yating
Zhang, Xiaomei
Hua, Lei
Guo, Yanlei
Yang, Yong
author_sort Wang, Yunhong
collection PubMed
description BACKGROUND: The aim of the present study is to increase the solubility of dihydroartemisinin (DHA) using the self-emulsifying drug delivery system (SEDDS). METHODS: We first conducted solubility test and ternary phase diagram, then, in order to optimize the formulation of the DHA self-emulsifying agent, the design mixture method was selected in the design expert software. Next, optimal prescription validation and preliminary formulation evaluation were conducted. By comparing the oil–water partition coefficient in vitro, the improvement of the in vivo osmotic absorption of DHA via self-emulsification was evaluated. RESULTS: The optimal prescription ratio of oleic acid polyethylene glycol glyceride, polyoxyethylene hydrogenated castor oil, and diethylene glycol monoethyl ether in the DHA self-emulsifying preparation = 0.511:0.2:0.289 (w/w/w), with a drug-loading capacity of 26.3634 mg/g, solubility of 2.5448 mg/ml, and self-emulsification time of 230 s. The solubility self-emulsification was approximately 20.52 × higher in DHA than in the crude drug. The self-emulsification could improve DHA permeability and promoting in vivo DHA absorption. CONCLUSION: The DHA SEDDS could significantly improve DHA solubility and in vivo absorption.
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spelling pubmed-91370712022-05-28 Oil–water partition coefficient preparation and detection in the dihydroartemisinin self-emulsifying drug delivery system Wang, Yunhong Chen, Jingcai Yang, Yang Gao, Sijia Wang, Zhuzhu Liu, Yating Zhang, Xiaomei Hua, Lei Guo, Yanlei Yang, Yong BMC Biotechnol Research BACKGROUND: The aim of the present study is to increase the solubility of dihydroartemisinin (DHA) using the self-emulsifying drug delivery system (SEDDS). METHODS: We first conducted solubility test and ternary phase diagram, then, in order to optimize the formulation of the DHA self-emulsifying agent, the design mixture method was selected in the design expert software. Next, optimal prescription validation and preliminary formulation evaluation were conducted. By comparing the oil–water partition coefficient in vitro, the improvement of the in vivo osmotic absorption of DHA via self-emulsification was evaluated. RESULTS: The optimal prescription ratio of oleic acid polyethylene glycol glyceride, polyoxyethylene hydrogenated castor oil, and diethylene glycol monoethyl ether in the DHA self-emulsifying preparation = 0.511:0.2:0.289 (w/w/w), with a drug-loading capacity of 26.3634 mg/g, solubility of 2.5448 mg/ml, and self-emulsification time of 230 s. The solubility self-emulsification was approximately 20.52 × higher in DHA than in the crude drug. The self-emulsification could improve DHA permeability and promoting in vivo DHA absorption. CONCLUSION: The DHA SEDDS could significantly improve DHA solubility and in vivo absorption. BioMed Central 2022-05-27 /pmc/articles/PMC9137071/ /pubmed/35624465 http://dx.doi.org/10.1186/s12896-022-00746-6 Text en © The Author(s) 2022 https://creativecommons.org/licenses/by/4.0/Open AccessThis article is licensed under a Creative Commons Attribution 4.0 International License, which permits use, sharing, adaptation, distribution and reproduction in any medium or format, as long as you give appropriate credit to the original author(s) and the source, provide a link to the Creative Commons licence, and indicate if changes were made. The images or other third party material in this article are included in the article's Creative Commons licence, unless indicated otherwise in a credit line to the material. If material is not included in the article's Creative Commons licence and your intended use is not permitted by statutory regulation or exceeds the permitted use, you will need to obtain permission directly from the copyright holder. To view a copy of this licence, visit http://creativecommons.org/licenses/by/4.0/ (https://creativecommons.org/licenses/by/4.0/) . The Creative Commons Public Domain Dedication waiver (http://creativecommons.org/publicdomain/zero/1.0/ (https://creativecommons.org/publicdomain/zero/1.0/) ) applies to the data made available in this article, unless otherwise stated in a credit line to the data.
spellingShingle Research
Wang, Yunhong
Chen, Jingcai
Yang, Yang
Gao, Sijia
Wang, Zhuzhu
Liu, Yating
Zhang, Xiaomei
Hua, Lei
Guo, Yanlei
Yang, Yong
Oil–water partition coefficient preparation and detection in the dihydroartemisinin self-emulsifying drug delivery system
title Oil–water partition coefficient preparation and detection in the dihydroartemisinin self-emulsifying drug delivery system
title_full Oil–water partition coefficient preparation and detection in the dihydroartemisinin self-emulsifying drug delivery system
title_fullStr Oil–water partition coefficient preparation and detection in the dihydroartemisinin self-emulsifying drug delivery system
title_full_unstemmed Oil–water partition coefficient preparation and detection in the dihydroartemisinin self-emulsifying drug delivery system
title_short Oil–water partition coefficient preparation and detection in the dihydroartemisinin self-emulsifying drug delivery system
title_sort oil–water partition coefficient preparation and detection in the dihydroartemisinin self-emulsifying drug delivery system
topic Research
url https://www.ncbi.nlm.nih.gov/pmc/articles/PMC9137071/
https://www.ncbi.nlm.nih.gov/pubmed/35624465
http://dx.doi.org/10.1186/s12896-022-00746-6
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