Formulation and Evaluation of Self-Micro Emulsifying Drug Delivery System for BCS Class - II Drug Ketoprofen

摘要

Ketoprofen, a widely prescribed analgesic drug which belongs to BCS class II and exhibit low and variable oral bioavailability due to its poor aqueous solubility. To enhance the solubility and dissolution rate of poorly water soluble drug Ketoprofen, Self-micro emulsifying drug delivery system (SMEDDS) was developed and evaluated. Solubility study, emulsification ability, ternary phase diagram and central composite design (CCD) were used as primary tools to select the components of the system and optimize the composition of liquid Ketoprofen SMEDDS. The globule size of optimized liquid SMEDDS was 105.08±5.16nm, zeta potential -4.23mV and polydispersity index 0.097, % Transmittance 98.45% and self emulsification time 28 sec. Optimized formulation F3 containing Oleic acid (10%), Tween 80 (30%) and Propylene glycol (60%) was adsorbed onto inert solid carrier Aerosil 200 in 1:1 ratio to form dry, free flowing powder. The liquid crystal phase viscosity increased significantly with increasing amount of aerosil 200 which in turn increases average globule size of solid SMEDDS (303.69±0.933nm) and slowers drug release. S-SMEDDS also characterized for DSC, XRD, SEM etc. The in vitro dissolution study indicates improved dissolution characteristics with higher percent drug release for solid SMEDDS (89.78%) compared to marketed preparation (81.26%) and pure drug (71.32%). In conclusion, S-SMEDDS for Ketoprofen holds promise to be developed as potential system for improved oral delivery.