Abstract
Naringenin (NRG) is a natural flavonoid compound abundantly present in citrus fruits and has the potential to treat respiratory disorders. However, the clinical therapeutic effect of NRG is limited by its low bioavailability due to poor solubility. To enhance the solubility, naringenin nanosuspensions (NRG-NSps) were prepared by applying tocopherol polyethylene glycol succinate (TPGS) as the nanocarrier via the media-milling method. The particle size, morphology, and drug-loading content of NRG-NSps were examined, and the stability was evaluated by detecting particle size changes in different physiological media. NRG-NSps exhibited a flaky appearance with a mean diameter of 216.9 nm, and the drug-loading content was 66.7%. NRG-NSps exhibited good storage stability and media stability. NRG-NSps presented a sustainable release profile, and the cumulative drug-release rate approached approximately 95% within 7 d. NRG-NSps improved the antitussive effect significantly compared with the original NRG, the cough frequency was decreased from 22 to 15 times, and the cough incubation period was prolonged from 85.3 to 121.6 s. Besides, NRG-NSps also enhanced expectorant effects significantly, and phenol red secretion was increased from 1.02 to 1.45 μg/mL. These results indicate that NRG-NSps could enhance the bioavailability of NRG significantly and possess a potential clinical application.
Highlights
Publisher’s Note: MDPI stays neutralNaringenin (NRG), an aglycone of naringin, belongs to the dihydroflavones and mainly exists in natural plants such as citrus, aurantium, peach leaf, and grapefruit [1].Studies have found that naringin has antibacterial [2], antioxidant and antiviral [3], and anticancer properties [4,5] that can inhibit the expression of pro-inflammatory cytokines [6], which have potential clinical applications for therapy for pulmonary diseases such as Staphylococcus aureus pneumonia, pulmonary fibrosis, and asthma [7]
Nanosuspensions, nanomicelles, nanoparticles, and nanocrystals are prepared with nanomaterials as nanocarriers to entrap hydrophobic drugs, and these nanodelivery systems could enhance the solubility of hydrophobic drugs in aqueous solution, further improving their with regard to jurisdictional claims in published maps and institutional affiliations
Institutional Review Board Statement: The study was conducted according to the ethical and regulatory guidelines approved by the Animal Ethics Committee of Peking Union Medical College (Beijing, China), the ethical approval number of this study is SLXD-20191231005 (31 December 2019)
Summary
Studies have found that naringin has antibacterial [2], antioxidant and antiviral [3], and anticancer properties [4,5] that can inhibit the expression of pro-inflammatory cytokines [6], which have potential clinical applications for therapy for pulmonary diseases such as Staphylococcus aureus pneumonia, pulmonary fibrosis, and asthma [7]. The solubility of naringin in water is very poor and almost insoluble, and the oral bioavailability of naringin is only 5.81%, which seriously affects its therapeutic effect and further restricts its clinical application [8]. The development of nanotechnology has provided new ideas for improving the solubility and bioavailability of hydrophobic drugs [9,10]. Nanosuspensions, nanomicelles, nanoparticles, and nanocrystals are prepared with nanomaterials as nanocarriers to entrap hydrophobic drugs, and these nanodelivery systems could enhance the solubility of hydrophobic drugs in aqueous solution, further improving their with regard to jurisdictional claims in published maps and institutional affiliations.
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