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

Abstract

The present work aimed to apply the liquid antisolvent precipitation (LAP) method for preparing the apigenin nanoparticles and thereby improving the solubility and bioavailability of apigenin. The different experimental parameters on particle size were optimized through central composite design (CCD) using the Design-Expert V R software. Under the optimum conditions, the particle size of the apigenin nanosuspension was about 159.2 nm. In order to get apigenin nanoparticles, the freeze-drying method was selected and the mannitol was used as a cryoprotectant. Then the solid state properties of the apigenin nanoparticles were investigated using scanning electron microscopy (SEM), differential scanning calorimetry (DSC), thermo gravimetric (TG), and X-ray diffraction (XRD). The results obtained displayed that the apigenin nanoparticles exhibited near-spherical shape and could be transformed into an amorphous form. In addition, the dissolving test, the bioavailability in rats, and the antitumor activity were also studied. The experimental results showed that the solubility of the apigenin nanoparticles were about 29.61 times and 64.81 times of raw apigenin in artificial gastric juice and in artificial intestinal juice, respectively, and the apigenin nanoparticles showed higher dissolution rates compared to raw apigenin, and was about 6.08 times and 6.14 times than that of raw apigenin in artificial gastric juice and in artificial intestinal juice. The oral bioavailability of apigenin nanoparticles was about 4.96 times higher than that of the raw apigenin, but the apigenin nanoparticles had no toxic effect on the organs of rats. In addition, the apigenin nanoparticles had a higher inhibition to HepG2 cells by lower IC50 than that of raw apigenin. ARTICLE HISTORY

Preparation, Characterization, and In Vivo Evaluation of Amorphous Icaritin Nanoparticles Prepared by a Reactive Precipitation Technique

“…However, our results revealed that AINs prepared by anti-solvent precipitation and sonoprecipitation methods yielded obvious crystals, as shown in Figure 6c. These findings are consistent with those of Wu et al [20], who prepared apigenin (a flavonoid compound) nanoparticles by anti-solvent precipitation and found that the resultant morphology was also in the form of crystals. Thus, our results indicate that these other commonly used methods did not work for preparing AINs.…”

“…These results indicated that soluplus and VA64 completely inhibited icaritin crystallization and promoted the formation of amorphous particles. Although the other four tested polymers (P188, P407, PEG4000, and CMC-Na) have been widely used to prepare amorphous particles [ 20 ], they did not work in our experiments for preparing AINs. In addition, we also measured the particle-size distributions of AINs prepared by different polymers.…”

Enhancing Oral Bioavailability of Apigenin Using a Bioactive Self-Nanoemulsifying Drug Delivery System (Bio-SNEDDS): In Vitro, In Vivo and Stability Evaluations

“…Potential benefits of SNEDDS technology for poorly soluble drugs are the nanosized particle, increased drug dissolution rate, increased rate and extent of absorption, and reduced variability under fed and fasted states. In addition, it offers various advantages over conventional dosage forms, including the reduction in the dose frequency and possible side effects [ 19 , 20 ].…”

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“…Several methods for improvement of the solubility of active moiety include nanosization by high shear mixing, uniform distribution and stabilization of drug by use of polymers or stabilizers, milling and antisolvent precipitation-ultrasonication 6,7 . Out of these, antisolvent precipitation-ultra-sonication technology is simple, economical, rapid, and straight forward 8 .…”