Preparation of Baicalein Long-Circulating Liposome and Its Effect on Bone Implantation in Diabetic Rats

Abstract

Gradual increase in blood glucose is the major characteristics of a metabolic disease like diabetes. Inflammatory microenvironment and diabetes induced osteoporosis seriously affect prognosis of patients that undergo bone implantation. Baicalein is a natural flavonoid compound with hypoglycemic, anti-inflammatory and other pharmacological functions. Clinically, the application of baicalein is hampered by inadequate solubility, low bioavailability and other shortcomings. In this report, we designed a long-circulating liposome for potential delivery of baicalein. The best formula for long-circulating liposome preparation was obtained by screening excipients, viz., Phospholipids:Cholesterol= 10:1, Phospholipids:DSPEPEG2000 = 6:1 and Phospholipids:Baicalein= 5:1. Respectively, average size of liposomal particles and encapsulation rate were approximately 190 nm and 91%. The drug release percentage within 24 h was 60%, amid being significantly better than that of the free drug. During in vivo pharmacokinetics experiment, we observed a significantly higher plasma baicalein concentration in mice of liposome group comparable to those in free drug group amid consistency with the drug release observation. It was confirmed through in vivo studies that baicalein long-circulating liposomes could reduce blood glucose and pro-inflammatory factors in rats, thus improving the state of liver, kidney and pancreas in diabetic model rats and significantly reversing diabetes induced osteoporosis.