Solubilization and changes of physicochemical properties of baicalin by nano sponge, and toxicity of zebrafish liver

As a new type of drug carrier, nano-sponge (NS) can remarkably improve the solubility of poorly soluble drug components, significantly increase the efficacy of drugs and their bioavailability. Baicalin (BA) has many biological activities, such as anti-inflammatory, bacteriostatic and etc. But due to its poor solubility, BA cannot play a role in the clinic. Therefore, it is urgent to find a suitable solubilization technology to improve the solubility of BA. In this paper, we optimized the preparation process of NS based on β-cyclodextrin (β-CD), and then prepared the baicalin nano-sponges (BA-NS). The successful preparation of BA-NS was verified by modern analysis methods. BA loading capacity and efficiency (BLC and BLE), solubilizing effect, in vitro release rate and liver toxicity were investigated. The results showed that the BLC and BLE were 18.02 ± 0.36% and 86.64 ± 0.86%, solubility in water was 31 times than that of pure BA, and release rate in different media could reach 80%. Zebrafish liver toxicity test showed no obvious toxicity. The above results showed that NS had a significant solubilizing effect on BA and was safe and non-toxic, and proved that NS maybe have broad prospects in the research of poorly soluble drugs.