Abstract
Author(s): P. Gota, A. Adegoke, M. Gurjar, S. Singh, M. Nandave, L. Hingorani and V. Gota*
Boswellic acids (BAs) including 11-keto-β-boswellic acid (KBA) and 3-acetyl-11-keto-β-boswellic acid (AKBA) are the active principles of Boswelliaserrata extract (BSE) which is used in traditional Indian medicine for the treatment of inflammatory conditions. BAs are characterized by low oral bioavailability. In order to circumvent this problem, solid lipid boswelliaserrata particles (SLBSP) were developed which is essentially a complexation of BAs with phospholipids such as phosphatidyl choline. The objective of this study was to compare the metabolic stability of SLBSP versus plain BSE using HHL-17, a Human telomere inactivated hepatocyte cell line. The two formulations were incubated in HHL-17 for time points ranging from 30 minutes to 480 minutes. At the end of incubation period, cells were lysed and concentration of KBA and AKBA in the cell lysates was estimated using a validated LC-MS/MS technique. It was observed that KBA from plain BSE was cleared by the hepatocytes with a half-life of 5.8 hours, whereas, KBA from SLBSP exhibited lesser accumulation in hepatocytes and lowmetabolic clearance. No difference was observed in the rate of metabolism of AKBA from the two formulations. It can be concluded that phospholipid complexation confers metabolic stability to KBA by rendering it less permeable into human hepatocytes.