Effect of multicomponent crystal of piperine-nicotinic acid on antihyperlipidemic activity in rats.

The alkaloid piperine is the main bioactive compound in black pepper (Piper nigrum L) and exhibits antihyperlipidemic activity. Piperine is a Biopharmaceutical Classification System (BCS) Class II compound, which has low water solubility, resulting in low bioavailability. This study aims to examine the effects of multicomponent nicotinic acid-piperine crystals on antihyperlipidemic activity in rats fed a high-fat diet. To increase the effectiveness of piperine, we prepared multicomponent crystals by the solvent-drop grinding method, using nicotinic acid as a co-former. The antihyperlipidemic activity of the preparation was estimated by measuring total cholesterol (TC), total triglycerides (TG), low-density lipoprotein cholesterol (LDLc) and high-density lipoprotein cholesterol (HDLc), using the enzymatic colorimetric method. Rats fed a high-fat diet exhibited an increase in plasma lipid levels. However, rats administered the multicomponent piperine-nicotinic acid crystals at a dose of 40 mg/kg/BW showed significantly (p<0.050) reduced plasma lipid levels. Compared with hyperlipidemic rats, multicomponent crystals of piperine-nicotinic acid decreased TC from 237.8±8.02 mg/dL to 174.53±7.07mg/dL, TG levels from 208.33±5.79 to 85.95±7.41mg/dL and LDLc levels from 144.225±15.99 mg/dL to 88.55±10.83mg/dL but increased HDLc levels from 51.93±10.92mg/dL to 68.78±2.56 mg/dL. Thus, the results demonstrate that the multicomponent piperine-nicotinic acid crystals lowered TC, TG and LDLc but increased HDLc.