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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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Influence of microemulsion incubation time on cellular morphology.
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f8-ijn-7-2465: Influence of microemulsion incubation time on cellular morphology.

Mentions: Various vehicles loaded with Evo and Rut affected cellular morphology (Figure 6). For all formulations, a concentration of 20% and an incubation time of 8 hours were used. Compared to normal cells, cells incubated with microemulsion (whether or not the microemulsion was loaded with drugs; Figures 6–8) showed no obvious changes. In addition, no morphologic change was noted in cells incubated with the aqueous suspension (Figure 6). The drugs (Evo and Rut) had no apparent effect on the cells at the dosage used, as shown by the similar cellular morphology seen in cells incubated with the microemulsion vehicle without drugs (Figures 6–8). However, cells incubated with the tincture shrank sharply and underwent necrocytosis (Figure 6), as indicated by the amount of cellular debris observed floating in the culture fluid. This effect may have been due to the high alcohol content of the tincture.


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)

Influence of microemulsion incubation time on cellular morphology.
© Copyright Policy
Related In: Results  -  Collection

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

f8-ijn-7-2465: Influence of microemulsion incubation time on cellular morphology.
Mentions: Various vehicles loaded with Evo and Rut affected cellular morphology (Figure 6). For all formulations, a concentration of 20% and an incubation time of 8 hours were used. Compared to normal cells, cells incubated with microemulsion (whether or not the microemulsion was loaded with drugs; Figures 6–8) showed no obvious changes. In addition, no morphologic change was noted in cells incubated with the aqueous suspension (Figure 6). The drugs (Evo and Rut) had no apparent effect on the cells at the dosage used, as shown by the similar cellular morphology seen in cells incubated with the microemulsion vehicle without drugs (Figures 6–8). However, cells incubated with the tincture shrank sharply and underwent necrocytosis (Figure 6), as indicated by the amount of cellular debris observed floating in the culture fluid. This effect may have been due to the high alcohol content of the tincture.

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