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In vitro cellular uptake of evodiamine and rutaecarpine using a microemulsion

OBJECTIVE: To investigate the cellular uptake of evodiamine and rutaecarpine in a microemulsion in comparison with aqueous suspensions and tinctures. MATERIALS AND METHODS: A microemulsion was prepared using the dropwise addition method. Mouse skin fibroblasts were cultured in vitro to investigate t...

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Autores principales: Zhang, Yong-Tai, Huang, Zhe-Bin, Zhang, Su-Juan, Zhao, Ji-Hui, Wang, Zhi, Liu, Ying, Feng, Nian-Ping
Formato: Online Artículo Texto
Lenguaje:English
Publicado: Dove Medical Press 2012
Materias:
Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC3367489/
https://www.ncbi.nlm.nih.gov/pubmed/22679361
http://dx.doi.org/10.2147/IJN.S30616
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author Zhang, Yong-Tai
Huang, Zhe-Bin
Zhang, Su-Juan
Zhao, Ji-Hui
Wang, Zhi
Liu, Ying
Feng, Nian-Ping
author_facet Zhang, Yong-Tai
Huang, Zhe-Bin
Zhang, Su-Juan
Zhao, Ji-Hui
Wang, Zhi
Liu, Ying
Feng, Nian-Ping
author_sort Zhang, Yong-Tai
collection PubMed
description OBJECTIVE: To investigate the cellular uptake of evodiamine and rutaecarpine in a microemulsion in comparison with aqueous suspensions and tinctures. MATERIALS AND METHODS: A microemulsion was prepared using the dropwise addition method. Mouse skin fibroblasts were cultured in vitro to investigate the optimal conditions for evodiamine and rutaecarpine uptake with different drug concentrations and administration times. Under optimal conditions, the cellular uptake of microemulsified drugs was assayed and compared to tinctures and aqueous suspensions. Rhodamine B labeling and laser scanning confocal microscopy (LSCM) were used to explore the distribution of fluorochrome transferred with the microemulsion in fibroblasts. Cellular morphology was also investigated, using optical microscopy to evaluate microemulsion-induced cellular toxicity. RESULTS: The maximum cellular drug uptake amounts were obtained with a 20% concentration (v/v) of microemulsion and an 8 hour administration time. Drug uptake by mouse skin fibroblasts was lowest when the drugs were loaded in microemulsion. After incubation with rhodamine B-labeled microemulsion for 8 hours, the highest fluorescence intensity was achieved, and the fluorochrome was primarily distributed in the cytochylema. No obvious cellular morphologic changes were observed with the administration of either the microemulsion or the aqueous suspension; for the tincture group, however, massive cellular necrocytosis was observed. CONCLUSION: The lower cellular uptake with microemulsion may be due to the fact that most of the drug loaded in the microemulsion vehicle was transported via the intercellular space, while a small quantity of free drug (released from the vehicle) was ingested through transmembrane transport. Mouse skin fibroblasts rarely endocytosed evodiamine and rutaecarpine with a microemulsion as the vehicle. The microemulsion had no obvious effect on cellular morphology, suggesting there is little or no cellular toxicity associated with the administration of microemulsion on mouse skin fibroblasts.
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spelling pubmed-33674892012-06-07 In vitro cellular uptake of evodiamine and rutaecarpine using a microemulsion Zhang, Yong-Tai Huang, Zhe-Bin Zhang, Su-Juan Zhao, Ji-Hui Wang, Zhi Liu, Ying Feng, Nian-Ping Int J Nanomedicine Original Research OBJECTIVE: To investigate the cellular uptake of evodiamine and rutaecarpine in a microemulsion in comparison with aqueous suspensions and tinctures. MATERIALS AND METHODS: A microemulsion was prepared using the dropwise addition method. Mouse skin fibroblasts were cultured in vitro to investigate the optimal conditions for evodiamine and rutaecarpine uptake with different drug concentrations and administration times. Under optimal conditions, the cellular uptake of microemulsified drugs was assayed and compared to tinctures and aqueous suspensions. Rhodamine B labeling and laser scanning confocal microscopy (LSCM) were used to explore the distribution of fluorochrome transferred with the microemulsion in fibroblasts. Cellular morphology was also investigated, using optical microscopy to evaluate microemulsion-induced cellular toxicity. RESULTS: The maximum cellular drug uptake amounts were obtained with a 20% concentration (v/v) of microemulsion and an 8 hour administration time. Drug uptake by mouse skin fibroblasts was lowest when the drugs were loaded in microemulsion. After incubation with rhodamine B-labeled microemulsion for 8 hours, the highest fluorescence intensity was achieved, and the fluorochrome was primarily distributed in the cytochylema. No obvious cellular morphologic changes were observed with the administration of either the microemulsion or the aqueous suspension; for the tincture group, however, massive cellular necrocytosis was observed. CONCLUSION: The lower cellular uptake with microemulsion may be due to the fact that most of the drug loaded in the microemulsion vehicle was transported via the intercellular space, while a small quantity of free drug (released from the vehicle) was ingested through transmembrane transport. Mouse skin fibroblasts rarely endocytosed evodiamine and rutaecarpine with a microemulsion as the vehicle. The microemulsion had no obvious effect on cellular morphology, suggesting there is little or no cellular toxicity associated with the administration of microemulsion on mouse skin fibroblasts. Dove Medical Press 2012 2012-05-18 /pmc/articles/PMC3367489/ /pubmed/22679361 http://dx.doi.org/10.2147/IJN.S30616 Text en © 2012 Zhang et al, publisher and licensee Dove Medical Press Ltd. This is an Open Access article which permits unrestricted noncommercial use, provided the original work is properly cited.
spellingShingle Original Research
Zhang, Yong-Tai
Huang, Zhe-Bin
Zhang, Su-Juan
Zhao, Ji-Hui
Wang, Zhi
Liu, Ying
Feng, Nian-Ping
In vitro cellular uptake of evodiamine and rutaecarpine using a microemulsion
title In vitro cellular uptake of evodiamine and rutaecarpine using a microemulsion
title_full In vitro cellular uptake of evodiamine and rutaecarpine using a microemulsion
title_fullStr In vitro cellular uptake of evodiamine and rutaecarpine using a microemulsion
title_full_unstemmed In vitro cellular uptake of evodiamine and rutaecarpine using a microemulsion
title_short In vitro cellular uptake of evodiamine and rutaecarpine using a microemulsion
title_sort in vitro cellular uptake of evodiamine and rutaecarpine using a microemulsion
topic Original Research
url https://www.ncbi.nlm.nih.gov/pmc/articles/PMC3367489/
https://www.ncbi.nlm.nih.gov/pubmed/22679361
http://dx.doi.org/10.2147/IJN.S30616
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