On the inherent properties of Soluplus and its application in ibuprofen solid dispersions generated by microwave-quench cooling technology

Abstract

Polyvinyl caprolactam-polyvinyl acetate-polyethylene glycol graft copolymer, or Soluplus^®, is a relatively new copolymer and a promising carrier of amorphous solid dispersions. Knowledge on the inherent properties of Soluplus^® (e.g. cloud points, critical micelle concentrations, and viscosity) in different conditions is relatively inadequate, and the application characteristics of Soluplus^®-based solid dispersions made by microwave methods still need to be clarified. In the present investigation, the inherent properties of a Soluplus^® carrier, including cloud points, critical micelle concentrations, and viscosity, were explored in different media and in altered conditions. Ibuprofen, a BCS class II non-steroidal anti-inflammatory drug, was selected to develop Soluplus^®-based amorphous solid dispersions using the microwave-quench cooling (MQC) method. Scanning electronic microscopy (SEM), differential scanning calorimetry (DSC), powder X-ray diffraction (PXRD), Raman spectroscopy (RS), and Fourier transform infrared spectroscopy (FT-IR) were adopted to analyze amorphous properties and molecular interactions in ibuprofen/Soluplus^® amorphous solid dispersions generated by MQC. Dissolution, dissolution extension, phase solubility, equilibrium solubility, and supersaturated crystallization inhibiting experiments were performed to elucidate the effects of Soluplus^® on ibuprofen in solid dispersions. This research provides valuable information on the inherent properties of Soluplus^® and presents a basic understanding of Soluplus^® as a carrier of amorphous solid dispersions.

Keywords:

• Soluplus^®
• inherent properties
• ibuprofen
• amorphous solid dispersions
• crystallization inhibition
• dissolution

Disclosure statement

The authors confirm that this article content has no conflicts of interest.

Funding

This work was supported by China Postdoctoral Science Foundation (No. 2015M571373), the NSFC (No. 81602654), Science and Technology Development Program of Jilin Province of China (No. 20160520046JH), Scientific Research Foundation of the Education Department of Jilin Province of China (No.2015–401), the State Key Laboratory of Medicinal Chemical Biology of Nankai University (No.201503001) and Science and Technology Development Program of Jilin city in Jilin Province of China (No. 201464053).