Stabilizing Effect of Soluplus on Erlotinib Metastable Crystal Form in Microparticles and Amorphous Solid Dispersions

Microparticles (MPs) and amorphous solid dispersions (SDs) are effective methods to improve the dissolution of insoluble drugs. However, stability is a concern for these two high-energy systems, resulting from high surface area and amorphous polymorph, respectively. As an amphiphilic polymer, Solupl...

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Bibliographic Details
Published in:Polymers 2022-03, Vol.14 (6), p.1241
Main Authors: Jia, Shuyu, Ning, Shangqi, Leng, Yuting, Jing, Qiufang, Xu, Zhongyu, Ren, Fuzheng
Format: Article
Language:English
Subjects:
Accelerated tests
Aqueous solutions
Bioavailability
Carbonyl groups
Carbonyls
Dispersions
Dissolution
Drugs
FDA approval
Fourier transforms
Hydrogen bonds
Infrared spectroscopy
Microparticles
Microscopy
Particle size
Polymers
Recrystallization
Solubilization
Solvents
Stability tests
Surfactants
System effectiveness
Thermogravimetric analysis
X ray powder diffraction
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Summary:Microparticles (MPs) and amorphous solid dispersions (SDs) are effective methods to improve the dissolution of insoluble drugs. However, stability is a concern for these two high-energy systems, resulting from high surface area and amorphous polymorph, respectively. As an amphiphilic polymer, Soluplus (SOL) is usually used as a carrier in SDs. In this study, erlotinib microparticles (ERL MPs) and erlotinib solid dispersions (ERL SDs) were prepared with SOL by bottom-up technology and solvent evaporation. The solid-state properties of ERL MPs and ERL SDs were characterized by Differential Scanning Calorimetry (DSC), Powder X-Ray Diffraction (PXRD) and Scanning Electron Microscopy (SEM). The ERL MPs existed in a metastable crystal form A while the ERL SDs existed in an amorphous state. Fourier transform infrared spectroscopy (FT-IR) showed that there was a hydrogen bond interaction between the N-H group of ERL and the carbonyl group of SOL in ERL MPs and SDs. The dissolution profiles of ERL SDs and ERL MPs were improved significantly. ERL MPs showed better stability than ERL SDs in accelerated stability test. The discrepant stabilizing effects of polymer SOL in two systems may provide effective ideas for solubilization of insoluble drugs and the stability of drugs after recrystallization.
ISSN:2073-4360
2073-4360
DOI:10.3390/polym14061241