Preparation of Vitexin Nanoparticles by Combining the Antisolvent Precipitation and High Pressure Homogenization Approaches Followed by Lyophilization for Dissolution Rate Enhancement

Abstract

Vitexin, a natural flavonoid found in many medicinal plants, is well known for its rich pharmacological activities. However, the poor water solubility of vitexin has limited its therapeutic application. The aim of this study was to prepare the nanoparticles of vitexin by combining the antisolvent precipitation (ASP) and high pressure homogenization (HPH) approaches followed by lyophilization for improving the dissolution rate of this poorly water-soluble drug. The effects of main factors influencing the mean particle size (MPS) of vitexin were investigated and optimized. Under optimum conditions, vitexin nanosuspensions with an MPS of 80.5 nm were obtained and then lyophilized to form nanoparticles. The obtained vitexin nanoparticles were further characterized by scanning electron microscopy (SEM), Fourier transform infrared spectroscopy (FTIR), mass spectrometry (MS), X-ray powder diffraction (XRPD), gas chromatography (GC) and dissolution testing. The results showed that the nanoparticles of vitexin were converted into an amorphous form, with its chemical structure unchanged. Additionally, the residual dimethyl sulfoxide (DMSO) is lower than the International Conference on Harmonization (ICH) limit for class 3 solvents. The dissolution rate of processed vitexin was significantly higher (5.58-fold) than that of raw drug. Overall, the combinative process we developed is an effective way to produce vitexin nanoparticles with markedly enhanced dissolution rate.

A Novel Sprague-Dawley Rat Model Presents Improved NASH/NAFLD Symptoms with PEG Coated Vitexin Liposomes

“…Recently, vitexin was established to alleviate the non-alcoholic fatty liver disease via activation of AMP-activated protein kinase (AMPK) that resulted in lipolysis and inhibition of lipogenesis [ 40 ]. However, the low aqueous solubility and poor bioavailability of vitexin limits its therapeutic window [ 37 , 41 , 42 ].…”

Characterization, culture medium optimization and antioxidant activity of an endophytic vitexin-producing fungus Dichotomopilus funicola Y3 from pigeon pea [Cajanus cajan (L.) Millsp.]

“…The HPLC‐ESI‐MS analysis conditions were based on the method as described previously (Gu et al . ). Briefly, chromatographic separations were achieved on a HIQ Sil C18 column (250 mm × 4·6 mm i.d., 5 μ m, Kya Tech, Hachioji City, Japan) maintained at 25°C.…”

“…The concentration of vitexin in samples was analysed by an Agilent 1260 series HPLC system (Agilent, San Jose, CA, USA), consisting of a G1312A binary pump. The chromatographic condition was described as previously (Gu et al 2017).Briefly, chromatographic separations were performed on a HIQ Sil C18 column (250 mm 9 4Á6 mm i.d., 5 lm, Kya Tech, Hachioji City, Japan) at 25°C with a mobile phase of methanol-water-formic acid (15:84Á99:0Á01, v/v/v) at a flow rate of 1 ml min À1 . UV detection was at 332 nm, and the sample injection volume was 20 ll.…”

“…An Agilent 1260 series HPLC system consisting of a G1312A binary pump, a 7725i manual injector, and a G1379A degasser was used for chromatographic analysis. The HPLC-ESI-MS analysis conditions were based on the method as described previously (Gu et al 2017). Briefly, chromatographic separations were achieved on a HIQ Sil C18 column (250 mm 9 4Á6 mm i.d., 5 lm, Kya Tech, Hachioji City, Japan) maintained at 25°C.…”

Fabrication and characterization of nanoemulsions for encapsulation and delivery of vitexin: antioxidant activity, storage stability and in vitro digestibility

“…1,3 Therefore, production methods or technologies that increase vitexin solubility require development. Previously, nano-complex and nanoparticles of vitexin were created to enhance its solubility, [3][4][5] but no studies have assessed the development of nanoemulsions as vitexin delivery systems. Therefore, considerable interest has been shown in fabricating vitexinloaded nanoemulsions as an alternative and effective delivery process.…”