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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.


Related in: MedlinePlus

Physical characterization of BCL-NEs: (A) size distribution, (B) appearance, and (C) TEM micrograph.Abbreviations: BCL, baicalein; NEs, nanoemulsions; TEM, transmission electron microscopy.
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f3-ijn-12-2923: Physical characterization of BCL-NEs: (A) size distribution, (B) appearance, and (C) TEM micrograph.Abbreviations: BCL, baicalein; NEs, nanoemulsions; TEM, transmission electron microscopy.

Mentions: Considering the merits of smaller particle size and less surfactants in oral drug delivery, the formulation was finally decided as 40 mg of BCL, 1,000 mg of hemp oil, 50 mg of PM, and 50 mg of sodium oleate emulsified with 20 mL of water. The resulting BCL-NEs possessed a particle size of 90.6 nm with a polydispersity index of 0.225 (Figure 3A). The ζ potential was determined to be −45.2 mV, showing them to be stable as colloidal dispersion system. BCL-NEs exhibited a high EE that was up to 99.31%. BCL-NEs were opalescent in appearance and took on a blue light upon dilution (Figure 3B). BCL-NEs presented a near-spherical morphology as observed by TEM (Figure 3C). The particle size judged from the scale bar (200 nm) accorded well with the hydrodynamic size measured based on dynamic light scattering.


Biocompatible nanoemulsions based on hemp oil and less surfactants for oral delivery of baicalein with enhanced bioavailability
Physical characterization of BCL-NEs: (A) size distribution, (B) appearance, and (C) TEM micrograph.Abbreviations: BCL, baicalein; NEs, nanoemulsions; TEM, transmission electron microscopy.
© Copyright Policy
Related In: Results  -  Collection

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

f3-ijn-12-2923: Physical characterization of BCL-NEs: (A) size distribution, (B) appearance, and (C) TEM micrograph.Abbreviations: BCL, baicalein; NEs, nanoemulsions; TEM, transmission electron microscopy.
Mentions: Considering the merits of smaller particle size and less surfactants in oral drug delivery, the formulation was finally decided as 40 mg of BCL, 1,000 mg of hemp oil, 50 mg of PM, and 50 mg of sodium oleate emulsified with 20 mL of water. The resulting BCL-NEs possessed a particle size of 90.6 nm with a polydispersity index of 0.225 (Figure 3A). The ζ potential was determined to be −45.2 mV, showing them to be stable as colloidal dispersion system. BCL-NEs exhibited a high EE that was up to 99.31%. BCL-NEs were opalescent in appearance and took on a blue light upon dilution (Figure 3B). BCL-NEs presented a near-spherical morphology as observed by TEM (Figure 3C). The particle size judged from the scale bar (200 nm) accorded well with the hydrodynamic size measured based on dynamic light scattering.

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