Enhancing In Vitro Bioavailability of Berberine by Incorporation of Beta–Cyclodextrin Complex into Solid Dispersion System

Berberine is widely used in Eastern countries thanks to low cost and various biological activities. However, low solubility has limited its bioavailability. The purpose of this study is to prepare and evaluate solid dispersion loading berberine—β-cyclodextrin complex to improve the effective treatment of berberine. Two techniques, inclusion complex and solid dispersion, are applied to increase the bioavailability of berberine for further applications. The inclusion complex is prepared by grinding berberine and β-cyclodextrin with various ratios. Solid dispersion loading berberine—β-cyclodextrin complex is fabricated from polyethylene glycol (PEG 6000) by melting completely and then spray-drying with lactose for powder formation. The complex and solid dispersion is evaluated about solubility and drug release in distilled water. Moreover, the final product is also analyzed with powder X-ray diffraction (PXRD). As a result, the complex which has ratio 1:1 between berberine and β-cyclodextrin expresses the highest solubility and optimal dissolution profiles in distilled water in comparison with pure berberine. Solid dispersion samples show many advantages in solubility and dissolution rate compared to pure berberine; the solubility reaches nearly three times over pure berberine. The results of the sample of incorporation of the β-cyclodextrin complex into solid dispersion have significant improvement compared to pure berberine. In general, solid dispersion containing berberine β-cyclodextrin complex expresses the considerable enhancement in vitro bioavailability of berberine. Hence, it could be applied as a promising system for improving the therapeutic treatment of berberine.