STABILITY AND TOXICITY PROFILE OF SOLUTION ENHANCED DISPERSION BY SUPERCRITICAL FLUIDS (SEDS) FORMULATED Andrographis paniculata EXTRACT

Abstract

The main objective was to evaluate the stability and toxicity of a Solution Enhanced Dispersion by Supercritical Fluids (SEDS) formulated A. paniculata extract that was intended for food applications. The best formulated SEDS A. paniculata extract with improved dissolution of andrographolide (data not shown) was obtained using 25 mg/mL A. paniculata extract (maceration in acetone) and 6 mg/mL Eudragit L100-55 with acetone as feed solvent at the following SEDS co-precipitation conditions: 150 bar, 40 C, 15 L/min CO 2 flow rate (1 bar, 25 C), 0.5 mL/min liquid feed flow. Sticky A. paniculata extract with 16% w/w andrographolide was transformed into SEDS co-precipitates concentrated with 20.4% w/w andrographolide. Only 20-30% of andrographolide was degraded after two-month storage under 5, 30, 45 C at 75% relative humidity (RH). About 30-60% of andrographolide was degraded after addition into drinking water, orange drink, soybean milk for a day. This would imply its unstable nature after being dispersed and wetted in liquid food. SEDS co-precipitate was found to be practically acetone-free (< 0.1 ppm) by Headspace Gas Chromatography-Mass Spectrometry (GC-MS). This showed the capability of the SEDS process in stripping off acetone. Higher cytotoxic potential of SEDS co-precipitates (LC 50 = 46.46 µg/mL) than extract (LC 50 = 150.45 µg/mL) was observed.

Acute oral toxicity evaluation of andrographolide self-nanoemulsifying drug delivery system (SNEDDS) formulation

“…[ 33 34 ] Furthermore, in pure compound, AND also reported did not exert significant toxicity sign both in acute and subacute studies. [ 35 ] Meanwhile, AND in SEDS formulation featured higher cytotoxic potential than in the extract[ 36 ] which verified that the formulation alter the toxicity profile.…”