Pegylated bilosomes for improvement of oral delivery of Biochanin A: Development to preclinical evaluation

Biochanin A (BC) is a natural herbal isoflavone compound and potentially benefits human health. It had poor solubility which led to poor bioavailability. The present work was to develop pegylated bilosomes (BSpeg) to enhance the therapeutic efficiency of BC. The BC-BSpeg was developed by the thin film hydration method and optimized by box-bhekhen design. The span-60, polyethylene glycol (PEG-2000SA), and bile salt (sodium deoxycholate) were taken as independent variables, whereas vesicle size (VS) and entrapment efficiency (EE) were taken as dependent variables. The optimized BC-BSpeg formulation had 216±6.62nm of VS, 80.54±1.02% of EE, 0.231 of PDI, and 15.4 (negative) of zeta potential. X-ray diffraction study showed the drug was encapsulated into a BS matrix. The optimized BC-BSpeg showed a prolonged release profile (88.23±3.54% in 24h) and high ex-vivo intestinal permeation (56.97 ± 2.76 % in 6h). The optimized BC-BSpeg exhibited 4.70-fold higher bioavailability than pure BC dispersion. The optimized BC-BSpeg formulation exhibited significantly higher anti-inflammatory activity at each time point than pure BC dispersion. It was suggested that pegylated BS might be a new carrier for BC that could improve its therapeutic activity.