Preparation and in vitro evaluation of hesperidin nanoparticles by antisolvent recrystallization in a double homogenate system.

Hesperidin nanoparticles (HNPs) were made for the first time employing an antisolvent recrystallization technique in a double homogenate system with positive and negative clockwise rotation in order to completely use the underutilized nutritional components in citrus peel. Dimethyl sulfoxide (DMSO), ethanol, and deionized water were used as the solvents and antisolvents in the hesperidin solution preparation. Hesperidin solution concentration of 60.26 mg/mL, homogenization speed of 8257 rpm, antisolvent-to-solvent volume ratio of 6.93 mL/mL, and homogenization time of 3.15 min were the ideal experimental conditions. HNPs have to be at least 72.24 nm in size. The structures of the produced hesperidin samples and the raw hesperidin powder were identical, according to the findings of the FTIR, XRD, and TG characterization tests. The HNP sample had an in vitro absorption rate that was 5.63 and 4.23 times greater than that of the raw hesperidin powder, respectively. It was discovered that DMSO was more suited than ethanol for creating HNP particles. In the realms of dietary supplements, therapeutic applications, and health promotion, the HNPs produced by the ARDH technology would be a potential formulation on increasing uses for a wider range of nutraceuticals (synergistic).

Naringenin Ultrafine Powder Was Prepared by a New Anti-Solvent Recrystallization Method.

Raw naringenin directly isolated from plants is significantly limited by its poor dissolution rate and low bioavailability for clinical and in vivo studies. This study reported a method for the preparation of naringenin ultrafine powder (NUP) using a novel anti-solvent recrystallization process; preliminary experiments were conducted using six single-factor experiments. The response surface Box-Behnken (BBD) design was used to optimize the level of factors. The optimal preparation conditions of the DMP were obtained as follows: the feed rate was 40.82 mL/min, the solution concentration was 20.63 mg/mL, and the surfactant ratio was 0.62%. The minimum average particle size was 305.58 ± 0.37 nm in the derived optimum conditions. A scanning electron microscope was used to compare and analyze the appearance and morphology of the powder before and after preparation. The characterization results of FTIR, TG and XRD showed that no chemical change occurred in the powder before and after preparation. Through the simulated gastrointestinal juice digestion experiment, it was confirmed that the absorption rate of NUP was 2.96 times and 4.05 times higher than raw naringenin, respectively. Therefore, the results showed that the reduction in the particle size through the use of low-speed recrystallization could improve the absorption rate and provided a feasible approach for the further applications.

In vitro dissolution enhancement of micronized l-nimodipine by antisolvent re-crystallization from its crystal form H.

In order to enhance solubility and dissolution rate in water, micronized l-nimodipine (NMD) has been successfully prepared by antisolvent re-crystallization process using acetone as solvent and deionized water as antisolvent. The effects of five experimental parameters on the mean particle size (MPS) of NMD nanosuspension were investigated. It was found that the MPS of NMD nanosuspension decreased significantly when the concentration of NMD-acetone solution increased from 50 to 150 mg/mL along with the increase of volume ratio of antisolvent to solvent from 1 to 3, and then increased slightly with the following increase of them. By contrast, the MPS decreased with the increased feed rate of NMD-acetone solution and the amount of surfactant, from 1 to 3 mL/min and 0.025% to 0.2%, respectively. Thereafter, the MPS did not show any obvious change. The precipitation temperature had no significant effects on MPS. The optimum micronization conditions were determined as follows: NMD-acetone solution concentration of 150 mg/mL, the volume ratio of antisolvent to solvent of 3, the flow rate of NMD-acetone solution of 9 mL/min, the preparation temperature of 15°C and the amount of the surfactant of 0.2%. Under optimum conditions, micronized NMD with a MPS of 708.3 nm was obtained. The micronized product was characterized using scanning electron microscopy (SEM), Fourier transform infrared spectroscopy (FTIR), high performance liquid chromatography-mass spectrometry (LC-MS), X-ray diffraction (XRD), differential scanning calorimetry (DSC), and thermo gravimetric (TG), to verify the influences of micronization process on the final product. The results showed that the chemical structure of micronized NMD was not changed, but the crystalline structure had undergone transition during precipitation, which changed from form H into L. The dissolution test showed that micronized NMD exhibited enhanced dissolution rate and solubility of 5.22 folds compared to raw H-NMD. These results suggested that micronized NMD may have potential value to become a new oral NMD formulation with high bioavailability.

Representation and in vitro transdermal characteristics of glycyrrhizic acid nanoparticles prepared by antisolvent recrystallization method / 中草药

Objective: To prepare glycyrrhizic acid nanoparticles (GAN) using ethanol as solvent and ethyl acetate as the antisolvent, and to investigate the osmosis of GAN as carrier of dermal administration. Methods: Using scanning electron microscope (SEM), laser particle size analyzer, Fourier transform-infrared spectroscopy (FT-IR), and release rate analysis, the untreated glycyrrhizic acid (GA) and GA powder were characterized; In vitro cutaneous permeation experiments were carried out on modified Franz diffusion cells, using excised mouse skin. The concentration of diammonium glycyrrhizinate in the receptor compartments and skin were determined by HPLC. Results: The GAN was spherical, the average particle size was 220 nm, and the dissolution rate of nanosized glycyrrhizinate was improved obviously. The transdermal rate of nanosized glycyrrhizinate was better than the original glycyrrhizin, and the 12 h unit accumulation transmissibility of GAN and GA was 78.51 and 9.792 μg/cm2, respectively. Conclusion: After preparing, the particle size becomes smaller, the chemical structure does not change significantly, and both of dissolution rate and in vitro transdermal performance have been improved. The GAN has the potential application values in the development of pharmaceutical industry.