Preparation, characterization and antitumor activity evaluation of apigenin nanoparticles by the liquid antisolvent precipitation technique

Figures & data

Figure 1. Chemical structure of apigenin.

Table 1. Summary of reports available on production of Apigenin particles.

Type	Production techniques used	Particle sizeobtained (nm)	Water solubility	Oral bioavailability improved (AUC values)	Reference
Apigenin nanocrystals	Combination technology (CT), i.e. bead milling and subsequently high-pressure homogenization	413	–	–	Al Shaal et al., 2011
Apigenin nanocrystals	SmartCrystal combination technology	3–3000	–	–	Al Shaal et al., 2010
Apigenin nanocrystals	Supercritical antisolvent process	400–800	–	3.4 times	Zhang et al., 2013
Apigenin-loaded liposomes	Lipid film hydration method	103.20 ± 2.1	–	–	Banerjee et al., 2017
Apigenin-loaded liposomes	Lipid film hydration method (slight modification)	104.3 ± 1.8	–	–	Banerjee et al., 2015
Apigenin-loaded tocopherol derivative-containing D-alpha-tocopheryl polyethylene glycol 1000 succinate (TPGS) liposomes	Lipid film hydration method (slight modification)	118.6 ± 8.1	–	–	Jin et al., 2017
Apigenin-loaded ethosome	Conventional mechanical dispersion	90.99 ± 2.20	–	–	Shen et al., 2014
Apigenin-loaded polymeric micelles	Thin-film dispersion method	16.9	320.8 μg/mL	–	Zhai et al., 2013
Apigenin-loaded mixed micelles	Ethanol thin-film hydration method	178.565	5.6165 mg/mL	4.03 times	Zhang et al., 2017
Apigenin-loaded W/O/W emulsions	Multilayer emulsion	910	–	4 times	Kim et al., 2016

Figure 2. SEM images; (A) raw apigenin; (B) apigenin nanoparticles.

Figure 3. The XRD results (A) DSC results (B) and TG results (C) of each sample. (a) raw apigenin; (b) apigenin nanoparticles; (c) physical mixture of apigenin and mannitol; (d) poloxamer; and (e) mannitol.

Figure 4. Dissolution results of the samples in artificial gastric juice (A) and artificial intestinal juice (B).

Figure 5. The plasma concentration (A) and the inhibitory rate (B) of raw apigenin and apigenin nanoparticles.

Al Shaal L, Shegokar R, Müller RH. (2011). Production and characterization of antioxidant apigenin nanocrystals as a novel UV skin protective formulation. Int J Pharm 420:133–40.

 PubMed Web of Science ®Google Scholar

Al Shaal L, Müller RH, Shegokar R. (2010). SmartCrystal combination technology: scale up from lab to pilot scale and long term stability. Pharmazie 65:877–84.

 PubMed Web of Science ®Google Scholar

Zhang J, Huang Y, Liu D, et al. (2013). Preparation of apigenin nanocrystals using supercritical antisolvent process for dissolution and bioavailability enhancement. Eur J Pharm Sci 48:740–7.

 PubMed Web of Science ®Google Scholar

Banerjee K, Banerjee S, Mandal M. (2017). Enhanced chemotherapeutic efficacy of apigenin liposomes in colorectal cancer based on flavone-membrane interactions. J Colloid Interface Sci 491:98–110.

 PubMed Web of Science ®Google Scholar

Banerjee K, Banerjee S, Das S, Mandal M. (2015). Probing the potential of apigenin liposomes in enhancing bacterial membrane perturbation and integrity loss. J Colloid Interface Sci 453:48–59.

 PubMed Web of Science ®Google Scholar

Jin X, Yang Q, Zhang Y. (2017). Synergistic apoptotic effects of apigenin TPGS liposomes and tyroservatide: implications for effective treatment of lung cancer. Ijn 12:5109–18.

 Web of Science ®Google Scholar

Shen LN, Zhang YT, Wang Q, et al. (2014). Enhanced in vitro and in vivo skin deposition of apigenin delivered using ethosomes. Int J Pharm 460:280–8.

 PubMed Web of Science ®Google Scholar

Zhai Y, Guo S, Liu C, et al. (2013). Preparation and in vitro evaluation of apigenin-loaded polymeric micelles. Colloids Surf A 429:24–30.

 Web of Science ®Google Scholar

Zhang Z, Cui C, Wei F, Lv H. (2017). Improved solubility and oral bioavailability of apigeninvia soluplus®/pluronic F127binary mixed micelles system. Drug Develop Ind Pharm 43:1.

 PubMed Web of Science ®Google Scholar

Kim BK, Cho AR, Park DJ. (2016). Enhancing oral bioavailability using preparations of apigenin-loaded W/O/W emulsions: in vitro and in vivo evaluations. Food Chem 206:85–91.

 PubMed Web of Science ®Google Scholar