Physico-mechanistic studies on effect of spray drying and corrective excipients on direct compressibility of nanosponges by SeDeM analysis.

Objectives: SeDeM analysis enables rapid screening of powders for direct compression (DC) into tablets. Aim of this work was to investigate plain nanosponges (NS) and spray dried nanosponges (SDNS) for direct compressibility using SeDeMExpert system. Beta-cyclodextrin (β-CD) based NS are widely used for solubility, stability enhancement, and taste masking. Evaluation of their compressibility profile will shorten timelines required for early formulation development studies of tablets excipients.

Methods: NS were synthesized by crosslinking β-CD with diphenyl carbonate (DPC) and spray dried. They were evaluated for spectral and particle characteristics and characterized by SeDeManalysis. Primary indices of dimension: compressibility, flowability, lubricity, and stability were calculated by converting the micromeritic properties into 'r' values using factors. Radar diagrams were plotted to map micromeritic properties. Avicel^® and Supertab^® were mixed with NS and SDNS to correct deficiencies.

Results: Spectral characterization confirmed formation of NS. SeDeManalysis and radar diagrams conveyed lacunae in powder characteristics. SDNS displayed better micromeritics than NS however compressibility index was deficient in both. Avicel^® and Supertab^® were mixed with NS and SDNS and SeDeM analysis of mixtures revealed superior micromeritic properties providing conclusive proof of direct compressibility. Index of good compressibility (IGC) of mixtures was above limits.

Conclusions: SeDeManalysis is promising technique to characterize powders and predict compressibility of powders. It provides pointers to need for particle engineering to facilitate DC.