Cargando…
Application of Soluplus to Improve the Flowability and Dissolution of Baicalein Phospholipid Complex
In this study, a novel ternary complex system (TCS) composed of baicalein, phospholipids, and Soluplus was prepared to improve the flowability and dissolution for baicalein phospholipid complex (BPC). TCS was characterized using differential scanning calorimetry (DSC), infrared spectroscopy (IR), po...
Autores principales: | , , , , |
---|---|
Formato: | Online Artículo Texto |
Lenguaje: | English |
Publicado: |
MDPI
2017
|
Materias: | |
Acceso en línea: | https://www.ncbi.nlm.nih.gov/pmc/articles/PMC6153996/ https://www.ncbi.nlm.nih.gov/pubmed/28492487 http://dx.doi.org/10.3390/molecules22050776 |
_version_ | 1783357610852876288 |
---|---|
author | Fan, Junting Dai, Yunhao Shen, Hongxue Ju, Jianming Zhao, Zhiying |
author_facet | Fan, Junting Dai, Yunhao Shen, Hongxue Ju, Jianming Zhao, Zhiying |
author_sort | Fan, Junting |
collection | PubMed |
description | In this study, a novel ternary complex system (TCS) composed of baicalein, phospholipids, and Soluplus was prepared to improve the flowability and dissolution for baicalein phospholipid complex (BPC). TCS was characterized using differential scanning calorimetry (DSC), infrared spectroscopy (IR), powder X-ray diffraction (PXRD), and scanning electron microscopy (SEM). The flowability, solubility, oil–water partition coefficient, in vitro dissolution, and in vivo pharmacokinetics of the system were also evaluated. DSC, IR, PXRD, and SEM data confirmed that the crystal form of baicalein disappeared in BPC and TCS. Furthermore, the angle of repose of TCS of 35° indicated an improvement in flowability, and solubility increased by approximately eight-fold in distilled water when TCS was compared with BPC (41.00 ± 4.89 μg/mL vs. 5.00 ± 0.16 μg/mL). Approximately 91.24% of TCS was released at the end of 60 min in 0.5% SDS (pH = 6.8), which suggested that TCS could improve the dissolution velocity and extent. Moreover, TCS exhibited a considerable enhancement in bioavailability with higher peak plasma concentration (25.55 μg/mL vs. 6.05 μg/mL) and increased AUC(0–∞) (62.47 μg·h/mL vs. 50.48 μg·h/mL) with 123.75% relative bioavailability compared with BPC. Thus, Soluplus achieved the purpose of improving the flowability and solubility of baicalein phospholipid complexes. The application of Soluplus to phospholipid complexes has great potential. |
format | Online Article Text |
id | pubmed-6153996 |
institution | National Center for Biotechnology Information |
language | English |
publishDate | 2017 |
publisher | MDPI |
record_format | MEDLINE/PubMed |
spelling | pubmed-61539962018-11-13 Application of Soluplus to Improve the Flowability and Dissolution of Baicalein Phospholipid Complex Fan, Junting Dai, Yunhao Shen, Hongxue Ju, Jianming Zhao, Zhiying Molecules Article In this study, a novel ternary complex system (TCS) composed of baicalein, phospholipids, and Soluplus was prepared to improve the flowability and dissolution for baicalein phospholipid complex (BPC). TCS was characterized using differential scanning calorimetry (DSC), infrared spectroscopy (IR), powder X-ray diffraction (PXRD), and scanning electron microscopy (SEM). The flowability, solubility, oil–water partition coefficient, in vitro dissolution, and in vivo pharmacokinetics of the system were also evaluated. DSC, IR, PXRD, and SEM data confirmed that the crystal form of baicalein disappeared in BPC and TCS. Furthermore, the angle of repose of TCS of 35° indicated an improvement in flowability, and solubility increased by approximately eight-fold in distilled water when TCS was compared with BPC (41.00 ± 4.89 μg/mL vs. 5.00 ± 0.16 μg/mL). Approximately 91.24% of TCS was released at the end of 60 min in 0.5% SDS (pH = 6.8), which suggested that TCS could improve the dissolution velocity and extent. Moreover, TCS exhibited a considerable enhancement in bioavailability with higher peak plasma concentration (25.55 μg/mL vs. 6.05 μg/mL) and increased AUC(0–∞) (62.47 μg·h/mL vs. 50.48 μg·h/mL) with 123.75% relative bioavailability compared with BPC. Thus, Soluplus achieved the purpose of improving the flowability and solubility of baicalein phospholipid complexes. The application of Soluplus to phospholipid complexes has great potential. MDPI 2017-05-11 /pmc/articles/PMC6153996/ /pubmed/28492487 http://dx.doi.org/10.3390/molecules22050776 Text en © 2017 by the authors. 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 (http://creativecommons.org/licenses/by/4.0/). |
spellingShingle | Article Fan, Junting Dai, Yunhao Shen, Hongxue Ju, Jianming Zhao, Zhiying Application of Soluplus to Improve the Flowability and Dissolution of Baicalein Phospholipid Complex |
title | Application of Soluplus to Improve the Flowability and Dissolution of Baicalein Phospholipid Complex |
title_full | Application of Soluplus to Improve the Flowability and Dissolution of Baicalein Phospholipid Complex |
title_fullStr | Application of Soluplus to Improve the Flowability and Dissolution of Baicalein Phospholipid Complex |
title_full_unstemmed | Application of Soluplus to Improve the Flowability and Dissolution of Baicalein Phospholipid Complex |
title_short | Application of Soluplus to Improve the Flowability and Dissolution of Baicalein Phospholipid Complex |
title_sort | application of soluplus to improve the flowability and dissolution of baicalein phospholipid complex |
topic | Article |
url | https://www.ncbi.nlm.nih.gov/pmc/articles/PMC6153996/ https://www.ncbi.nlm.nih.gov/pubmed/28492487 http://dx.doi.org/10.3390/molecules22050776 |
work_keys_str_mv | AT fanjunting applicationofsoluplustoimprovetheflowabilityanddissolutionofbaicaleinphospholipidcomplex AT daiyunhao applicationofsoluplustoimprovetheflowabilityanddissolutionofbaicaleinphospholipidcomplex AT shenhongxue applicationofsoluplustoimprovetheflowabilityanddissolutionofbaicaleinphospholipidcomplex AT jujianming applicationofsoluplustoimprovetheflowabilityanddissolutionofbaicaleinphospholipidcomplex AT zhaozhiying applicationofsoluplustoimprovetheflowabilityanddissolutionofbaicaleinphospholipidcomplex |