Cargando…
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...
Autores principales: | , , , , , |
---|---|
Formato: | Online Artículo Texto |
Lenguaje: | English |
Publicado: |
MDPI
2022
|
Materias: | |
Acceso en línea: | https://www.ncbi.nlm.nih.gov/pmc/articles/PMC8949943/ https://www.ncbi.nlm.nih.gov/pubmed/35335571 http://dx.doi.org/10.3390/polym14061241 |
_version_ | 1784675024253222912 |
---|---|
author | Jia, Shuyu Ning, Shangqi Leng, Yuting Jing, Qiufang Xu, Zhongyu Ren, Fuzheng |
author_facet | Jia, Shuyu Ning, Shangqi Leng, Yuting Jing, Qiufang Xu, Zhongyu Ren, Fuzheng |
author_sort | Jia, Shuyu |
collection | PubMed |
description | 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. |
format | Online Article Text |
id | pubmed-8949943 |
institution | National Center for Biotechnology Information |
language | English |
publishDate | 2022 |
publisher | MDPI |
record_format | MEDLINE/PubMed |
spelling | pubmed-89499432022-03-26 Stabilizing Effect of Soluplus on Erlotinib Metastable Crystal Form in Microparticles and Amorphous Solid Dispersions Jia, Shuyu Ning, Shangqi Leng, Yuting Jing, Qiufang Xu, Zhongyu Ren, Fuzheng Polymers (Basel) Article 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. MDPI 2022-03-19 /pmc/articles/PMC8949943/ /pubmed/35335571 http://dx.doi.org/10.3390/polym14061241 Text en © 2022 by the authors. https://creativecommons.org/licenses/by/4.0/Licensee MDPI, Basel, Switzerland. This article is an open access article distributed under the terms and conditions of the Creative Commons Attribution (CC BY) license (https://creativecommons.org/licenses/by/4.0/). |
spellingShingle | Article Jia, Shuyu Ning, Shangqi Leng, Yuting Jing, Qiufang Xu, Zhongyu Ren, Fuzheng Stabilizing Effect of Soluplus on Erlotinib Metastable Crystal Form in Microparticles and Amorphous Solid Dispersions |
title | Stabilizing Effect of Soluplus on Erlotinib Metastable Crystal Form in Microparticles and Amorphous Solid Dispersions |
title_full | Stabilizing Effect of Soluplus on Erlotinib Metastable Crystal Form in Microparticles and Amorphous Solid Dispersions |
title_fullStr | Stabilizing Effect of Soluplus on Erlotinib Metastable Crystal Form in Microparticles and Amorphous Solid Dispersions |
title_full_unstemmed | Stabilizing Effect of Soluplus on Erlotinib Metastable Crystal Form in Microparticles and Amorphous Solid Dispersions |
title_short | Stabilizing Effect of Soluplus on Erlotinib Metastable Crystal Form in Microparticles and Amorphous Solid Dispersions |
title_sort | stabilizing effect of soluplus on erlotinib metastable crystal form in microparticles and amorphous solid dispersions |
topic | Article |
url | https://www.ncbi.nlm.nih.gov/pmc/articles/PMC8949943/ https://www.ncbi.nlm.nih.gov/pubmed/35335571 http://dx.doi.org/10.3390/polym14061241 |
work_keys_str_mv | AT jiashuyu stabilizingeffectofsoluplusonerlotinibmetastablecrystalforminmicroparticlesandamorphoussoliddispersions AT ningshangqi stabilizingeffectofsoluplusonerlotinibmetastablecrystalforminmicroparticlesandamorphoussoliddispersions AT lengyuting stabilizingeffectofsoluplusonerlotinibmetastablecrystalforminmicroparticlesandamorphoussoliddispersions AT jingqiufang stabilizingeffectofsoluplusonerlotinibmetastablecrystalforminmicroparticlesandamorphoussoliddispersions AT xuzhongyu stabilizingeffectofsoluplusonerlotinibmetastablecrystalforminmicroparticlesandamorphoussoliddispersions AT renfuzheng stabilizingeffectofsoluplusonerlotinibmetastablecrystalforminmicroparticlesandamorphoussoliddispersions |