NERDG 2026
Poster 17 Abstract
Spray drying of poorly water-soluble drugs without any organic solvent using the acid-base supersolubilization (ABS) principle
Ajinkya Khedekar, Vishvesh Raje, Hari Priya Kandagatla, Mufaddal H Kathawala, Ketan Patel, Abu T. M. Serajuddin
Department of Pharmaceutical Sciences, College of Pharmacy and Health Sciences, St. John's University, Jamaica, NY 11439, USA
Presenting Author: Ajinkya Khedekar
Corresponding Author: Abu T. M. Serajuddin, [email protected]
Abstract
Over two-thirds of New Chemical Entities (NCE’s) are classified as BCS Class II or IV, requires solubilization strategies such as Amorphous Solid Dispersions (ASDs) to overcome bioavailability barriers. ASDs can be manufactured using spray drying which depends heavily on hazardous organic solvents, creating significant environmental, safety, and cost burdens due to the physicochemical difficulty of simultaneously dissolving hydrophobic drugs and hydrophilic polymers in same medium. This study uses the Acid-Base Supersolubilization (ABS) principle as a novel, organic-solvent-free alternative. Application of this principle to the model drug indomethacin using tromethamine achieved a solubility from <1 mg/mL to >240 mg/mL in aqueous media, enabling processing using water as the sole solvent. Solid-state characterization via Differential Scanning Calorimetry (DSC) and Powder X-ray Diffraction (PXRD) confirmed that aqueous spray drying successfully generated amorphous dispersions comparable to those produced by Hot-Melt Extrusion (HME), evidenced by the complete absence of characteristic crystalline peaks and melting endotherms. In comparative dissolution studies under acidic conditions (pH 1.0), the aqueous spray-dried ASD exhibited superior initial release kinetics, achieving >85% drug release within 15 minutes, significantly outpacing the HME formulation (80% after 45 minutes) due to optimized particle size distribution6. Although the spray-dried system showed transient precipitation after 60 minutes (~65% remaining in solution at 120 minutes), a pH transition to 6.8 resulted in immediate, complete, and sustained dissolution for both formulations. Ultimately, the ABS principle effectively circumvents the thermodynamic limitations of conventional spray drying, offering a transformative "green technology" platform that eliminates organic solvents while ensuring high solubility and rapid dissolution profiles.
Keywords
Acid–Base Supersolubilization (ABS); Spray Drying; Organic Solvent-Free; Amorphous Solid Dispersions; Weakly Acidic Drugs; Poorly Water-Soluble Drugs
Poster 17 Abstract
Spray drying of poorly water-soluble drugs without any organic solvent using the acid-base supersolubilization (ABS) principle
Ajinkya Khedekar, Vishvesh Raje, Hari Priya Kandagatla, Mufaddal H Kathawala, Ketan Patel, Abu T. M. Serajuddin
Department of Pharmaceutical Sciences, College of Pharmacy and Health Sciences, St. John's University, Jamaica, NY 11439, USA
Presenting Author: Ajinkya Khedekar
Corresponding Author: Abu T. M. Serajuddin, [email protected]
Abstract
Over two-thirds of New Chemical Entities (NCE’s) are classified as BCS Class II or IV, requires solubilization strategies such as Amorphous Solid Dispersions (ASDs) to overcome bioavailability barriers. ASDs can be manufactured using spray drying which depends heavily on hazardous organic solvents, creating significant environmental, safety, and cost burdens due to the physicochemical difficulty of simultaneously dissolving hydrophobic drugs and hydrophilic polymers in same medium. This study uses the Acid-Base Supersolubilization (ABS) principle as a novel, organic-solvent-free alternative. Application of this principle to the model drug indomethacin using tromethamine achieved a solubility from <1 mg/mL to >240 mg/mL in aqueous media, enabling processing using water as the sole solvent. Solid-state characterization via Differential Scanning Calorimetry (DSC) and Powder X-ray Diffraction (PXRD) confirmed that aqueous spray drying successfully generated amorphous dispersions comparable to those produced by Hot-Melt Extrusion (HME), evidenced by the complete absence of characteristic crystalline peaks and melting endotherms. In comparative dissolution studies under acidic conditions (pH 1.0), the aqueous spray-dried ASD exhibited superior initial release kinetics, achieving >85% drug release within 15 minutes, significantly outpacing the HME formulation (80% after 45 minutes) due to optimized particle size distribution6. Although the spray-dried system showed transient precipitation after 60 minutes (~65% remaining in solution at 120 minutes), a pH transition to 6.8 resulted in immediate, complete, and sustained dissolution for both formulations. Ultimately, the ABS principle effectively circumvents the thermodynamic limitations of conventional spray drying, offering a transformative "green technology" platform that eliminates organic solvents while ensuring high solubility and rapid dissolution profiles.
Keywords
Acid–Base Supersolubilization (ABS); Spray Drying; Organic Solvent-Free; Amorphous Solid Dispersions; Weakly Acidic Drugs; Poorly Water-Soluble Drugs
