Journal
EUROPEAN JOURNAL OF PHARMACEUTICAL SCIENCES
Volume 164, Issue -, Pages -Publisher
ELSEVIER
DOI: 10.1016/j.ejps.2021.105882
Keywords
Panax notoginseng saponins; Zein; Lipoprotein; Nanoparticles; Oral bioavailability
Categories
Funding
- National Natural Science Foundation of China [81673830]
- Six Talent Peaks Project of Jiangsu Province [YY053]
- Major Project and Double First-Class Innovative Team [CPU2018GY28]
- National Science and Technology Major Project [2017zx09101001005]
Ask authors/readers for more resources
The study developed PLZ-NPs for enhanced oral absorption of Panax Notoginseng Saponins (PNS) with improved stability and enzymolysis resistance. PLZ-NPs showed higher permeability, absorption efficiency, and oral bioavailability compared to free PNS, making it a promising approach for PNS analogues.
Panax Notoginseng Saponins (PNS) has been widely used in the prevention and treatment of cardiovascular and cerebrovascular diseases such as myocardial infarction, heart failure and cerebral infarction. However, oral administration of PNS showed low bioavailability because of its instability and poor membrane permeability in the gastrointestinal tract. Here, lipoprotein-inspired hybrid nanoparticles of PNS-Lecithin-Zein (PLZ-NPs) were prepared by using a simple phase separation method, which possessed a core-shell structure, where zein was used as protein part to replace the animal origin protein to increase the resistance to acid and enzymes while lecithin was used as the lipid composition to improve the oral absorption of PNS as well as to increase the drug loading capacity of PNS into the nanocarriers. The results of stability test showed that PLZ-NPs had robust enzymolysis resistance ability for acid and digestive enzymes of gastrointestinal environments. The fluorescent resonance energy transfer (FRET) assay confirmed the ability of LZ-NPs to be intactly absorbed by Caco-2 cell monolayer. Cell transport studies demonstrated that the permeability of PLZ-NPs in Caco-2/HT29-MTX co-culture cell model was 1.5-fold that of PNS. Meanwhile, the single-pass intestinal perfusion assay proved the absorption parameter Peff of PLZ-NPs was 1.75 and 1.80 times higher than that of PNS in the ileum and jejunum, respectively. Finally, the in vivo pharmacokinetic experiment showed that the relative oral bioavailability of PLZ-NPs was 1.71-fold that of free PNS in SD rat. In summary, the employment of the Lecithin/Zein hybrid nanoparticles could be considered as a promising approach for PNS analogues.
Authors
I am an author on this paper
Click your name to claim this paper and add it to your profile.
Reviews
Recommended
No Data Available