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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...

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Autores principales: Fan, Junting, Dai, Yunhao, Shen, Hongxue, Ju, Jianming, Zhao, Zhiying
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
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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.
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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
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