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In vitro cellular uptake of evodiamine and rutaecarpine using a microemulsion.

Zhang YT, Huang ZB, Zhang SJ, Zhao JH, Wang Z, Liu Y, Feng NP - Int J Nanomedicine (2012)

Bottom Line: Under optimal conditions, the cellular uptake of microemulsified drugs was assayed and compared to tinctures and aqueous suspensions.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.

View Article: PubMed Central - PubMed

Affiliation: Department of Pharmaceutics, Shanghai University of Traditional Chinese Medicine, Shanghai, The People's Republic of China.

ABSTRACT

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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Effect of microemulsion concentration on the amount of Evo (blue) and Rut (red) uptake by mouse skin fibroblasts.
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f3-ijn-7-2465: Effect of microemulsion concentration on the amount of Evo (blue) and Rut (red) uptake by mouse skin fibroblasts.

Mentions: Five concentrations of microemulsion liquid (5%, 10%, 15%, 20%, and 30%; v/v) were evaluated in this study. The results showed that the amount of uptake increased with increases in the microemulsion concentration and began to taper after the microemulsion accounted for 20% of the culture fluid (Figure 3). Within a concentration range of 5%–20%, the uptake amounts for Evo and Rut were dose dependent, indicating that cellular uptake may occur via passive transport. High microemulsion concentrations increased the concentration of the drugs in the culture fluid, but an excess of microemulsion components (eg, surfactant and cosurfactant) may hinder cellular uptake.


In vitro cellular uptake of evodiamine and rutaecarpine using a microemulsion.

Zhang YT, Huang ZB, Zhang SJ, Zhao JH, Wang Z, Liu Y, Feng NP - Int J Nanomedicine (2012)

Effect of microemulsion concentration on the amount of Evo (blue) and Rut (red) uptake by mouse skin fibroblasts.
© Copyright Policy
Related In: Results  -  Collection

Show All Figures
getmorefigures.php?uid=PMC3367489&req=5

f3-ijn-7-2465: Effect of microemulsion concentration on the amount of Evo (blue) and Rut (red) uptake by mouse skin fibroblasts.
Mentions: Five concentrations of microemulsion liquid (5%, 10%, 15%, 20%, and 30%; v/v) were evaluated in this study. The results showed that the amount of uptake increased with increases in the microemulsion concentration and began to taper after the microemulsion accounted for 20% of the culture fluid (Figure 3). Within a concentration range of 5%–20%, the uptake amounts for Evo and Rut were dose dependent, indicating that cellular uptake may occur via passive transport. High microemulsion concentrations increased the concentration of the drugs in the culture fluid, but an excess of microemulsion components (eg, surfactant and cosurfactant) may hinder cellular uptake.

Bottom Line: Under optimal conditions, the cellular uptake of microemulsified drugs was assayed and compared to tinctures and aqueous suspensions.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.

View Article: PubMed Central - PubMed

Affiliation: Department of Pharmaceutics, Shanghai University of Traditional Chinese Medicine, Shanghai, The People's Republic of China.

ABSTRACT

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.

Show MeSH
Related in: MedlinePlus