Enhanced bioavailability of apigenin via preparation of a carbon nanopowder solid dispersion

Abstract

In this study, a novel carbon nanopowder (CNP) drug carrier was developed to improve the oral bioavailability of apigenin (AP). Solid dispersions (SDs) of AP with CNP were prepared, and their in vitro drug release and in vivo performance were evaluated. The physicochemical properties of the formulations were examined by differential scanning calorimetry, X-ray diffraction, and scanning electron microscopy. Drug release profiles showed that AP dissolution from the CNP-AP system (weight ratio, 6:1) after 60 minutes improved by 275% compared with that of pure AP. Moreover, the pharmacokinetic analysis of SD formulations in rats showed that the AP area under the curve 0–t value was 1.83 times higher for the CNP-AP system than for pure AP, indicating that its bioavailability was significantly improved. In addition, compared with pure AP, SDs had a significantly higher peak and shorter time to peak. Preliminary intestinal toxicity tests indicated that there was no significant difference in the tissues of the rats treated with the CNP-AP system, rats treated with the CNP alone, and controls. In conclusion, CNP-based SDs could be used for enhancing the bioavailability of poorly water-soluble drugs while also improving drug safety.

Natural plant flavonoid apigenin directly disrupts Hsp90/Cdc37 complex and inhibits pancreatic cancer cell growth and migration

“…It would still be a challenge to prove our molecular study results using in vivo animal models in our future work, since apigenin only exhibited moderate solubility in lipid (0.001-1.63 mg/mL) and water (2.16 µg/mL in water) (Ding et al, 2014). However, numerous in vivo studies revealed that apigenin showed ideal bioactivities in animal models given oral administration.…”

Plant Flavone Apigenin: an Emerging Anticancer Agent

“…Formulations using carbon nanopowder solid dispersions for apigenin have proven to enhance its bioavailability. These apigenin nanoparticles showed low levels of toxicity in animals [236]. Apigenin-loaded lipid nanocapsules prepared with phase inversion method showed high efficacy in restricting breast and liver cancer growth [237].…”

Beneficial effects of celery (Apium graveolens) on metabolic syndrome: A review of the existing evidences

“…These challenges could be overcomed by new "lipid-based nano-encapsulation approaches" for targeted delivery of these functional compounds (Esfanjani, Assadpour, & Jafari, 2018). Innovative technologies such as nanocrystals, lipid-based nanoparticles including liposomes, phytosomes, micelles, solid lipid nanoparticles, microemulsions, and nanoemulsions, and solubility enhancing agents such as cyclodextrin have been reported for improvement of beneficial effects of celery's compounds (Dang et al, 2014;Ding, Zhang, et al, 2014;Huang et al, 2016;Khan, Saraf, & Saraf, 2016;Kim, Cho, & Park, 2016;Luo et al, 2019;Mahalapbutr et al, 2019;Shi, Zhao, Firempong, & Xu, 2016;Shin et al, 2018;Telange et al, 2017;Wu, Li, Yue, Zhang, & Yunusi, 2018;Wu et al, 2017;Zhai et al, 2013;Zhang, Huang, Liu, Gao, & Qian, 2013;Zhang, Cui, Wei, & Lv, 2017;Zhao, Wang, & Li, 2016). The effects of celery on metabolic syndrome are shown in Figure 2.…”