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

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

Pharmacokinetic profiles of BCL in Sprague-Dawley rats following oral administration of BCL suspensions, BCL conventional emulsions, and BCL-NEs (n=6, mean ± StD).Abbreviations: BCL, baicalein; NEs, nanoemulsions; StD, standard deviation.
© Copyright Policy
Related In: Results  -  Collection

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

f5-ijn-12-2923: Pharmacokinetic profiles of BCL in Sprague-Dawley rats following oral administration of BCL suspensions, BCL conventional emulsions, and BCL-NEs (n=6, mean ± StD).Abbreviations: BCL, baicalein; NEs, nanoemulsions; StD, standard deviation.

Mentions: The pharmacokinetic profiles of BCL following oral administration of various formulations are shown in Figure 5, and the main pharmacokinetic parameters are listed in Table 2. The formulation of suspensions brought about poor absorption of BCL both in the rate and the extent. The maximum plasma concentration (Cmax) and area under the plasma concentration–time curve (AUC0–t) were just 1.43 μg/mL and 7.96 μg h/mL, respectively. Compared with the formulation of BCL suspensions, the conventional emulsions, to a certain extent, promoted the oral absorption of BCL, resulting in an apparent improvement in the blood drug concentration. The finding suggests that lipid-based formulation can enhance the oral bioavailability of BCL. However, in the case of BCL-NEs, a dramatic enhancement in the oral absorption of BCL was achieved. BCL-NEs yielded higher blood BCL concentration at each time point. The Cmax and AUC0–t were separately up to 10.96 μg/mL and 41.77 μg h/mL, respectively. The oral bioavailability of BCL-NEs was calculated to be 524.7 and 242.1% relative to the suspensions and conventional emulsions, respectively. In terms of the time to maximum plasma concentration (Tmax), two kinds of emulsions were similar (~2 h) but different from the formulation of suspensions. In addition, the terminal half-life (T1/2) among three formulations was significantly distinct. These results indicate that there are differences in the absorption rate of BCL as formulated in different modalities. In contrast, NEs possessed a greater advantage in enhancing the oral absorption of BCL.


Biocompatible nanoemulsions based on hemp oil and less surfactants for oral delivery of baicalein with enhanced bioavailability
Pharmacokinetic profiles of BCL in Sprague-Dawley rats following oral administration of BCL suspensions, BCL conventional emulsions, and BCL-NEs (n=6, mean ± StD).Abbreviations: BCL, baicalein; NEs, nanoemulsions; StD, standard deviation.
© Copyright Policy
Related In: Results  -  Collection

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

f5-ijn-12-2923: Pharmacokinetic profiles of BCL in Sprague-Dawley rats following oral administration of BCL suspensions, BCL conventional emulsions, and BCL-NEs (n=6, mean ± StD).Abbreviations: BCL, baicalein; NEs, nanoemulsions; StD, standard deviation.
Mentions: The pharmacokinetic profiles of BCL following oral administration of various formulations are shown in Figure 5, and the main pharmacokinetic parameters are listed in Table 2. The formulation of suspensions brought about poor absorption of BCL both in the rate and the extent. The maximum plasma concentration (Cmax) and area under the plasma concentration–time curve (AUC0–t) were just 1.43 μg/mL and 7.96 μg h/mL, respectively. Compared with the formulation of BCL suspensions, the conventional emulsions, to a certain extent, promoted the oral absorption of BCL, resulting in an apparent improvement in the blood drug concentration. The finding suggests that lipid-based formulation can enhance the oral bioavailability of BCL. However, in the case of BCL-NEs, a dramatic enhancement in the oral absorption of BCL was achieved. BCL-NEs yielded higher blood BCL concentration at each time point. The Cmax and AUC0–t were separately up to 10.96 μg/mL and 41.77 μg h/mL, respectively. The oral bioavailability of BCL-NEs was calculated to be 524.7 and 242.1% relative to the suspensions and conventional emulsions, respectively. In terms of the time to maximum plasma concentration (Tmax), two kinds of emulsions were similar (~2 h) but different from the formulation of suspensions. In addition, the terminal half-life (T1/2) among three formulations was significantly distinct. These results indicate that there are differences in the absorption rate of BCL as formulated in different modalities. In contrast, NEs possessed a greater advantage in enhancing the oral absorption 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