Preparation of Berberine Chloride Nanoparticles by Ball Milling Method

Berberine is a quaternary benzylisoquinoline alkaloid that has been used for the local treatment of gastrointestinal tract diseases. Recently, several pharmacological effects of berberine have been reported, which include anti-hypertension, antitumor, anti-hypercholesterolemia, and neuroprotective effects. However, berberine has exhibited poor aqueous solubility and low oral bioavailability. To overcome these limitations, this study aims to develop and investigate nano berberine. Nano berberine fabricated by ball milling method is a simple process and easily applied in the production scale. The characterization of nano berberine was evaluated, including appearance, particle size, potential zeta, dissolution in vitro in a phosphate buffer media (pH 6.8), differential scanning calorimetry (DSC) analysis, fourier transformed infrared spectroscopy (FTIR), and X-ray diffraction analysis (XRD). Results from this study showed that spray-dried nano berberine powder was almost uniform in size, particle size average of 570.7 nm, and potential zeta of -28.6 mV. The dissolution in vitro study revealed that nano berberine was about 2 times more soluble than raw berberine for 60 minutes. No incompatibility between drug and excipients can be observed through FTIR and DSC analysis. XRD analysis suggested that raw berberine and nano berberine might exist in a crystal form. Thus, findings from this study indicate that the physicochemical properties of spray-dried nano berberine may increase the bioavailability of oral berberine. 
 