Large-Scale Synthesis and Comprehensive Validation of 2-Hydroxypropyl-β-Cyclodextrin Equivalent to Commercial Product

This study was a development from a previous study, which established the method for synthesizing 2-hydroxypropyl-β-cyclodextrin (HPβCD) from β-cyclodextrin and successfully applied it in large-scale production. The large-scale synthesis of HPβCD produced 1.38 ± 0.05 kg of 2-Hydroxypropyl-β-cyclodextrin, yielding 86.77 ± 0.68%, and a degree of substitution of 5.91. The synthesis was monitored using thin-layer chromatography. The synthesized product was then structurally characterized using infrared spectroscopy, nuclear magnetic resonance spectroscopy, and mass spectroscopy, along with the commercial HPβCD. As a comparative analysis, the spectroscopic data revealed no significant structural differences between the synthesized HPβCD and a commercially available counterpart. These findings validate the developed synthesis method, highlighting its potential for industrial application and future research into the uses of HPβCD in drug development. HIGHLIGHTS Successful Large-Scale Synthesis: A previously established method for synthesizing 2-hydroxypropyl-β-cyclodextrin (HPβCD) from β-cyclodextrin was successfully scaled up to achieve 1.38 ± 0.05 kg, yielding a high yield of 86.77 ± 0.68% and a degree of substitution of 5.91. Comprehensive Characterization: The synthesized HPβCD was rigorously monitored using thin-layer chromatography and structurally characterized by infrared spectroscopy, nuclear magnetic resonance (NMR) spectroscopy, and mass spectroscopy. Validation for Industrial Application: Comparative spectroscopic analysis against a commercial standard confirmed no significant structural differences, thereby validating the potential of this synthesis method for industrial application and future pharmaceutical research into HPβCD’s utility. GRAPHICAL ABSTRACT