Physicochemical and pharmacokinetic evaluation of rosuvastatin loaded nanostructured lipid carriers: influence of long- and medium-chain fatty acid mixture

Abstract

Combination of long and medium chain lipids show different behavior in-vivo and contribute differently for bioavailability. Aim of the present study was to evaluate the effect of long chain- (LCFA) and medium-chain (MCFA) fatty acid lipids on the bioavailability of rosuvastatin from rosuvastatin loaded nanostructured lipid carrier (RNLC). Lauric acid and capryol-90™ were selected as MCFA whereas stearic acid and oleic acid were chosen as LCFA. RNLC was prepared using melt-emulsification–ultrasonication method using different combinations of MCFA and LCFA. Non-ionic, non-toxic MYS-25 was used as stabilizing agent. RNLC showed entrapment efficiency of 85–92% denoting it to be beneficial for prolonged release of drug after oral administration. Zeta potential of −26.79 mV signifies particle stability through the repulsive forces which prevents aggregation upon storage. In-vivo oral pharmacokinetic study demonstrated six to ninefold improvement in the bioavailability of rosuvastatin (RSVS) in the form of RNLC than RSVS-Aqueous dispersion. A 1.5-fold increase in bioavailability was observed when RNLC was prepared with LCFA solid lipid and MCFA liquid lipid combination as compared to RNLC prepared using only MCFA as both solid and liquid lipid. Use of LCFA and MCFA combination was found to be superior as lipid mixture for the RNLC.