Abstract
To improve the water solubility and dissolution rate, genipin was nanocrystallized by an emulsion solvent evaporation method, followed by freeze‐drying. The optimization condition of nanocrystallization process was carried out by single‐factor experiment. The effects of five experimental parameters, such as concentration of surfactants the proportion of water to organic phase, homogenate speed and time, homogenization pressure and times, and the proportion of genipin to lyoprotectants on the mean particle size (MPS) of genipin nanoparticles, were investigated. Under the optimum conditions by single‐factor experiments, genipin nanoparticles with an MPS of 59.8 nm were obtained. The genipin nanoparticles were characterized by SEM, FTIR, XRD, DSC, solvent residue, drug purity test, dissolution testing, and bioavailability analysis. The analysis results indicated that the chemical structure of genipin nanoparticles was unchanged, but the crystallinity was reduced. The solubility of genipin nanoparticles was 9.05 times of the raw drug. In addition, the residual amounts of chloroform and ethanol were separately less than the ICH limit for class II, and the oral bioavailability of the genipin nanoparticles powder was 7.99 times of raw genipin. According to the results above, genipin nanoparticles show the potential application value of its oral absorption.
Highlights
Genipin (Figure 1) is an active compound, derived from iridoid glycosides-geniposidic (GENIPOSIDE) in the fruit of Gardenia
Genipin was nanocrystallized by an emulsion solvent evaporation method to further improve its dissolution rate and solubility, which to our knowledge has been unused in the previous experiments until now
10 mg of genipin nanoparticles were dissolved by 1 mL methanol and centrifuged at 8000 rpm for 5 min, and 1 μL samples were manually injected in split mode, with a split ratio of 20 : 1. The flow rate of hydrogen gas was 30 and that of air was 400 mL⋅min−1, respectively
Summary
Genipin (Figure 1) is an active compound, derived from iridoid glycosides-geniposidic (GENIPOSIDE) in the fruit of Gardenia. The application of genipin in oral administration is restricted as a result of poor aqueous solubility and low dissolution rate. These are the main barriers for the wide use of genipin in pharmaceutical formulations. Various methods have been used to improve dissolution, aqueous solubility, and bioavailability of poorly soluble drugs Such as preparation of nanoparticles [11], the use of solubilizer and surfactants [12], and the formation of solid dispersions [13, 14]. Genipin was nanocrystallized by an emulsion solvent evaporation method to further improve its dissolution rate and solubility, which to our knowledge has been unused in the previous experiments until now. The raw genipin and the optimized genipin nanoparticles were, respectively, characterized by SEM, FTIR, XRD, DSC, high-performance liquid chromatography (HPLC), dissolution test, residual solvent determination [27], and bioavailability tests [28]
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