Pharmacokinetics of solid lipid particles in healthy subjects.

OBJECTIVES

The anti-inflammatory activity of extracts (BSE) is well known. BSE comprises boswellic acids (BA) such as 3--acetyl-11-keto--boswellic acid (AKBA) and 11--boswellic acid (KBA) as major constituents. One of the limitations of BAs is their poor oral bioavailability. The aim of the study was to prepare solid lipid particles of extract (SLBSP) to enhance the bioavailability of BAs.

METHODS

The pharmacokinetic profile of BAs was studied in 10 healthy human volunteers following a single oral dose of 333 mg of SLBSP. Pharmacokinetic blood samples were collected at 0.5, 1, 1.5, 2, 2.5, 3, 4, 5, 6, 8, and 12 h post drug administration. Plasma KBA and AKBA levels were measured using a validated LC-MS/MS method. Pharmacokinetics parameters were estimated using Pheonix WinNonlin (Build 6.4.0.768) software.

RESULTS

Ten healthy human volunteers were included and peak plasma concentration was achieved in 1.5 and 2.3 h for AKBA and KBA respectively. Maximum plasma concentration () was 8.04 ± 1.67 ng/mL for AKBA and 23.83 ± 4.41 ng/mL for KBA whereas the corresponding area under the concentration-time curve (AUC) was 136.7 ± 56.77 ng/mLh and 165.7 ± 24.5 ng/mLh respectively. The elimination half-life () of AKBA and KBA was 6.8 ± 3.0 h and 2.45 ± 0.3 h respectively.

CONCLUSIONS

The SLBSP formulation of BSE showed enhanced oral bioavailability of BAs compared with historically reported data of unformulated BSE.