Enhancing Solubility of BCS Class II Drugs Using Melt Sonocrystallization: Formulation, Optimization, and Characterization of Dapsone Agglomerates.

Abstract

This work focusses on a BCS category II medication and presents a novel method for the synthesis, development, and characterisation of melt sonocrystallized (MSC) agglomerates. BCS category II medicines have poor bioavailability because of their increased permeability and lesser solubility, which makes formulation difficult. The medication chosen for study is dapsone, which belongs to the BCS Class II group and is well-known for its antitubercular pharmacological class. A potential method for increasing medication solubility and dissolving rates was melt sonocrystallization. The parameters of the melt sonocrystallization process, such as sonication time and amplitude, were optimised using a methodical approach. The MSC agglomerates were made by melting 500 mg of dapsone in a water bath, then adding it to 40 ml of deionised water at 50ºC and sonicating it using a probe sonicator. The suspension was filtered and dried in an oven. Drug release and content were compared using a three-level, two-factor factorial design for design of experiment (DoE) optimization. SEM, XRD, and FTIR were among the analytical methods utilised to characterise the created melt sonocrystallized agglomerates after the optimised batch was further formed into tablets. When compared to the drug's pure form, these methods showed better flow characteristics. To ascertain solubility and the proportion of drug release from agglomeration, an in-vitro dissolving research was conducted. The BCS category II medication's dissolution rate is considerably increased after melt sonocrystallization, according to the dissolution trials. In terms of agglomerates, this improvement was unmistakably demonstrating the increased surface area and decreased particle size, enabling quick release of active compounds. Overall, study highlights the potential of melt sonocrystallization as a viable strategy for enhancing the solubility as well as dissolution characteristics about BCS category II drugs, ultimately improving their bioavailability and therapeutic efficacy. This research contributes to advancing pharmaceutical formulation technologies to address challenges concerned with poorly soluble drugs, benefiting patient treatment outcomes and drug development endeavors.