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

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.

Small molecule inhibitors of epithelial‐mesenchymal transition for the treatment of cancer and fibrosis

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“…Fortunately, there are multiple ways to enhance the bioavailability, such as cocrystallization and the formation of phospholipid complexes and nanoemulsions. [215][216][217] Finally, based on the hypothesis that drugs targeting EMT have both antifibrotic and anticancer effects, many important mediators contributing to EMT have been discovered. Additionally, a great number of compounds suppress EMT in tumor and fibrosis by targeting these mediators.…”

Nanodelivery systems and stabilized solid-drug nanoparticles for orally administered medicine: current landscape

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Microfluidization trends in the development of nanodelivery systems and applications in chronic disease treatments

“…Recently various nanodelivery systems were developed using plant bioactive compounds like nanoemulsion or nanoparticles for their effective preventive role against various chronic diseases including cardiovascular effects. [172][173][174][175] Recently, Baicalein-loaded nanoemulsion was developed with a particle size of about 91 nm, showing excellent bioavailability of these compounds in rats, 176 and it could be possibly used in anticardiovascular studies. Another potential anticardiovascular compound β-carotene was studied using the microfluidization technique, and are able to produce food grade nanoemulsion along with higher stability with a particle size of ,200 nm.…”

“…Another potential anticardiovascular compound β-carotene was studied using the microfluidization technique, and are able to produce food grade nanoemulsion along with higher stability with a particle size of ,200 nm. 176 However, the enhanced stability of those active compound loaded nanodelivery systems developed using microfluidization techniques are still limited in their protective role in the anticardiovascular effects.…”