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Biocompatible nanoemulsions based on hemp oil and less surfactants for oral delivery of baicalein with enhanced bioavailability

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ABSTRACT

Baicalein (BCL) possesses high pharmacological activities but low solubility and stability in the intestinal tract. This study aimed to probe the potential of nanoemulsions (NEs) consisting of hemp oil and less surfactants in ameliorating the oral bioavailability of BCL. BCL-loaded NEs (BCL-NEs) were prepared by high-pressure homogenization technique to reduce the amount of surfactants. BCL-NEs were characterized by particle size, entrapment efficiency (EE), in vitro drug release, and morphology. Bioavailability was studied in Sprague-Dawley rats following oral administration of BCL suspensions, BCL conventional emulsions, and BCL-NEs. The obtained NEs were ~90 nm in particle size with an EE of 99.31%. BCL-NEs significantly enhanced the oral bioavailability of BCL, up to 524.7% and 242.1% relative to the suspensions and conventional emulsions, respectively. BCL-NEs exhibited excellent intestinal permeability and transcellular transport ability. The cytotoxicity of BCL-NEs was documented to be low and acceptable for oral purpose. Our findings suggest that such novel NEs and preparative process provide a promising alternative to current formulation technologies and suitable for oral delivery of drugs with bioavailability issues.

No MeSH data available.


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Cellular uptake of free BCL and BCL-NEs determined by the intracellular drug level (A) (mean ± StD, n=3) and cellular internalization of BCL-NEs evaluated by the CLSM imaging (B). *P<0.05; **P<0.01.Abbreviations: BCL, baicalein; CLSM, confocal laser scanning microscopy; NEs, nanoemulsions; StD, standard deviation.
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f6-ijn-12-2923: Cellular uptake of free BCL and BCL-NEs determined by the intracellular drug level (A) (mean ± StD, n=3) and cellular internalization of BCL-NEs evaluated by the CLSM imaging (B). *P<0.05; **P<0.01.Abbreviations: BCL, baicalein; CLSM, confocal laser scanning microscopy; NEs, nanoemulsions; StD, standard deviation.

Mentions: Figure 6A shows the cellular uptake of free BCL and BCL-NEs with the incubation time. There existed a significant difference in the cellular uptake between free BCL and encapsulated BCL. In the first time point (0.5 h), free BCL was taken up by Caco-2 cells, a little quicker than BCL-NEs. This may be connected with the high concentration of BCL surrounding the cells due to complete exposure. However, after that, the cellular uptake rate of BCL was accelerated by NEs compared with free BCL. The total uptake quantity of BCL-NEs was 1.86-fold as much as that of free BCL at 4 h. BCL-NEs resulted in higher BCL uptake, showing them to be promising in facilitating the transcellular transport of BCL.


Biocompatible nanoemulsions based on hemp oil and less surfactants for oral delivery of baicalein with enhanced bioavailability
Cellular uptake of free BCL and BCL-NEs determined by the intracellular drug level (A) (mean ± StD, n=3) and cellular internalization of BCL-NEs evaluated by the CLSM imaging (B). *P<0.05; **P<0.01.Abbreviations: BCL, baicalein; CLSM, confocal laser scanning microscopy; NEs, nanoemulsions; StD, standard deviation.
© Copyright Policy
Related In: Results  -  Collection

License 1 - License 2
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getmorefigures.php?uid=PMC5391827&req=5

f6-ijn-12-2923: Cellular uptake of free BCL and BCL-NEs determined by the intracellular drug level (A) (mean ± StD, n=3) and cellular internalization of BCL-NEs evaluated by the CLSM imaging (B). *P<0.05; **P<0.01.Abbreviations: BCL, baicalein; CLSM, confocal laser scanning microscopy; NEs, nanoemulsions; StD, standard deviation.
Mentions: Figure 6A shows the cellular uptake of free BCL and BCL-NEs with the incubation time. There existed a significant difference in the cellular uptake between free BCL and encapsulated BCL. In the first time point (0.5 h), free BCL was taken up by Caco-2 cells, a little quicker than BCL-NEs. This may be connected with the high concentration of BCL surrounding the cells due to complete exposure. However, after that, the cellular uptake rate of BCL was accelerated by NEs compared with free BCL. The total uptake quantity of BCL-NEs was 1.86-fold as much as that of free BCL at 4 h. BCL-NEs resulted in higher BCL uptake, showing them to be promising in facilitating the transcellular transport of BCL.

View Article: PubMed Central - PubMed

ABSTRACT

Baicalein (BCL) possesses high pharmacological activities but low solubility and stability in the intestinal tract. This study aimed to probe the potential of nanoemulsions (NEs) consisting of hemp oil and less surfactants in ameliorating the oral bioavailability of BCL. BCL-loaded NEs (BCL-NEs) were prepared by high-pressure homogenization technique to reduce the amount of surfactants. BCL-NEs were characterized by particle size, entrapment efficiency (EE), in vitro drug release, and morphology. Bioavailability was studied in Sprague-Dawley rats following oral administration of BCL suspensions, BCL conventional emulsions, and BCL-NEs. The obtained NEs were ~90 nm in particle size with an EE of 99.31%. BCL-NEs significantly enhanced the oral bioavailability of BCL, up to 524.7% and 242.1% relative to the suspensions and conventional emulsions, respectively. BCL-NEs exhibited excellent intestinal permeability and transcellular transport ability. The cytotoxicity of BCL-NEs was documented to be low and acceptable for oral purpose. Our findings suggest that such novel NEs and preparative process provide a promising alternative to current formulation technologies and suitable for oral delivery of drugs with bioavailability issues.

No MeSH data available.


Related in: MedlinePlus