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QbD BASED CONTROL STRATEGY OF LORATADINE NANOSUSPENSIONS AND DRY NANOPARTICLES STABILIZED BY SOLUPLUS®

AREEN ALSHWEIAT, RITA AMBRUS ^*, GÁBOR KATONA, ILDIKÓ CSÓKA

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The preparation of nanosuspensions has been introduced as a well-defined method to enhance the solubility and dissolution of poorly water-soluble drugs. The aim of this study was to evaluate the feasibility of using Soluplus® as a stabilizer for loratadine nanosuspensions. The concept of Quality by design (QbD) was followed particularly to link the critical material parameters (CMPs) and the critical process parameters (CPPs) with the required critical quality attributes (CQAs) and risk assessment (RA) to select the optimized critical material and process parameters. The ultrasonic-assisted precipitation method was selected to prepare the nanosuspensions with different concentrations of Soluplus®. Particle size, polydispersity index (PDI), solubility and dissolution were set as the main CQAs. Soluplus® successfully produced loratadine nanosuspensions with particle size ranging between 168.3 - 245.35 nm and PDI in the range of 0.12 and 0.25. The freeze dried sample with 0.6% Soluplus® (DLNS3) showed an amorphous status of loratadine with particle size and PDI in the range of 220 ± 6.23 and 0.21 ± 0.02, respectively. Contact angles, surface free energy, and polarity measurements showed an enhancement of the hydrophilic properties of DLNS3. DLNS3 displayed 121-fold saturation solubility and released approximately 57% of loratadine within 15 min. The effects of CMPs and CPPs on the CQA were expected by the QbD approach.