Background: FR&D scientists continuously try to increase the in vivo performance of low
soluble and bioavailable drugs. Solid SMEDDS and liquisolid formulations are relatively simple to
develop and fall within the novel drug delivery approaches. Here, a comparison is made to know relative
Objective: The study aimed to conduct comparative pharmacokinetic (PK) and pharmacodynamic (PD)
studies of developed Fluvastatin (FLU) solid SMEDDS (SSMED) and liquisolid formulation (LS) for
their relative in vivo efficacy.
Method: FLU liquid SMEDDS were optimized by central composite design (CCD). Components, oil,
surfactant and co-surfactant were selected as variables; particle size, self-emulsifying time and % drug
release in 15min were selected as responses. L-SMEDDS with positive charge inducer were adsorbed
on to porous carriers and characterized. Liquisolid formulations were prepared with Avicel PH-102 and
Neusilin US2 as carriers.
Results: Optimized L-SMEDDS contained 24.92 mg of oil, 45.18 mg of surfactant and 34.28 mg of cosurfactant.
SSMEDs containing Syloid XDP (SSMED-XDP) as carrier was selected based on flow
properties and liquid retention potential. The average particle size of SSMED-XDP was 154.30±1.10
nm, PDI was 0.311±0.03 and ZP was +19.57±1.34 mV after dilution. The drug release from SSMEDXDP
and LS formulations was higher than FLU powder. The bioavailability of SSMEDs was increased
by 3.00 fold and that of LS by 1.49 fold more than FLU-suspension. SSMEDs showed 12 h, while LS
and suspension showed only 6 h lipid-lowering effect.
Conclusion: The development of solid SMEDDS resulted in superior performance in both PK and PD
effects over the LS formulation.