Development and Statistical Optimization of Aquasomes Containing Ketoprofen: 2-Factor 2-Level Factorial Design Approach

Purpose: The purpose of the research work was to develop Aquasomes containing Ketoprofen (AQ-KP) for enhanced stability of the drug with improved therapeutic effect. Materials and Methods: The aquasomes are formulated by co-precipitation method using calcium phosphate as a core layer, lactose and cellulose as core coated layer. Ketoprofen was adsorbed on lactose and cellulose layers. The three-layer formulations are developed with varying concentration of lactose and cellulose for preliminary trial. A total of six aquasomal Formulations (F-1 to F-6) were developed and assessed for particle size, PDI, entrapment efficiency, In vitro release study. The best preliminary trial Formulation (F-6) was selected for statistical optimization using 22 factorial designs. In this, input variables were X1 (concentration of ethanol), X2 (stirring time) and output variables were Y1 (Entrapment efficiency %) and Y2 (In vitro release%). The optimized formulation (R-4) is further evaluated for particle size, PDI, SEM, XRD and DSC analysis. Results: The results of the optimized formulation showed that 63.7±1.4% of entrapment efficiency and 75.8±0.96% of in vitro release up to 8 hr. The scanning electron microscope showed a nearly spherical shape with rough texture. The X-ray diffraction study rooted the crystalline nature of the drug indicating that the drug is stable in aquasomal formulations. The release kinetic study demonstrates that the formulation followed case II transport. Conclusion: AQ-KP was successfully developed and optimized. These study results revealed that the aquasomes may have the potential for effective therapy with enhanced stability of drug.