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Scutellaria baicalensis Extract-phospholipid Complex: Preparation and Initial Pharmacodynamics Research in Rats

BACKGROUND: Baicalin, a flavonoid glycoside compound present in Scutellaria baicalensis, has shown a wide spectrum of biological activities, but its liposolubility, water-solubility and mucosal permeability are all very poor, which leads to the low concentration in brain and poor bioavailability by...

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Autores principales: Chen, Shibin, Xie, Qiujie, Yang, Ming, Shi, Yajun, Shi, Junhui, Zeng, Xiaobin
Formato: Online Artículo Texto
Lenguaje:English
Publicado: Bentham Science Publishers 2022
Materias:
Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC9189737/
https://www.ncbi.nlm.nih.gov/pubmed/34376131
http://dx.doi.org/10.2174/1389201022666210729142257
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author Chen, Shibin
Xie, Qiujie
Yang, Ming
Shi, Yajun
Shi, Junhui
Zeng, Xiaobin
author_facet Chen, Shibin
Xie, Qiujie
Yang, Ming
Shi, Yajun
Shi, Junhui
Zeng, Xiaobin
author_sort Chen, Shibin
collection PubMed
description BACKGROUND: Baicalin, a flavonoid glycoside compound present in Scutellaria baicalensis, has shown a wide spectrum of biological activities, but its liposolubility, water-solubility and mucosal permeability are all very poor, which leads to the low concentration in brain and poor bioavailability by oral or intravenous injective administration. OBJECTIVES: The primary objective of this study was to formulate the Scutellaria baicalensis extract (SBE) with phospholipid to yield Scutellaria baicalensis extract-phospholipid complex (SBEPC), and to evaluate its pharmacodynamics in the middle cerebral artery occlusion (MCAO). METHODS: The optimal preparation technology of SBEPC was obtained through single-factor test and central composite design-response surface methodology (CCD-RSM), and was characterized with various analytical techniques including SEM, FT-IR and NMR. The storage conditions of SBEPC were established through stability study and the MCAO rat model was investigated through conducting pharmacodynamic studies to screen the appropriate administration and dose of SBEPC as well as to verify the neuroprotective effect of SBEPC on cerebral ischemia-reperfusion injury. RESULTS: The optimized preparation conditions of SBEPC were summarized as follows: the ratio of phospholipids to drug was 2:1, the drug concentration was 3.5 mg/ml, the reaction temperature was 50 °C, and the entrapment efficiency was over 93.00%. Stability studies have demonstrated that SBEPC should be stored under 40 °C in a dry and ventilated place away from light and below 37% humidity. Furthermore, pharmacodynamic studies have found that, compared with SBE, SBEPC could introduce drugs into the brain and better exert the neuroprotective effect on MCAO rats, and the optimal administration and dose concentration of SBEPC were nasal administration and 40 mg/ml, respectively. CONCLUSION: These findings demonstrate that SBEPC is successfully prepared by CCD-RSM. SBEPC can enhance drugs' ability to enter the brain and improve the bioavailability of drugs in brain, and can effectively exert the neuroprotective effect on cerebral ischemia-reperfusion injury as compared with SBE.
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spelling pubmed-91897372022-06-27 Scutellaria baicalensis Extract-phospholipid Complex: Preparation and Initial Pharmacodynamics Research in Rats Chen, Shibin Xie, Qiujie Yang, Ming Shi, Yajun Shi, Junhui Zeng, Xiaobin Curr Pharm Biotechnol Article BACKGROUND: Baicalin, a flavonoid glycoside compound present in Scutellaria baicalensis, has shown a wide spectrum of biological activities, but its liposolubility, water-solubility and mucosal permeability are all very poor, which leads to the low concentration in brain and poor bioavailability by oral or intravenous injective administration. OBJECTIVES: The primary objective of this study was to formulate the Scutellaria baicalensis extract (SBE) with phospholipid to yield Scutellaria baicalensis extract-phospholipid complex (SBEPC), and to evaluate its pharmacodynamics in the middle cerebral artery occlusion (MCAO). METHODS: The optimal preparation technology of SBEPC was obtained through single-factor test and central composite design-response surface methodology (CCD-RSM), and was characterized with various analytical techniques including SEM, FT-IR and NMR. The storage conditions of SBEPC were established through stability study and the MCAO rat model was investigated through conducting pharmacodynamic studies to screen the appropriate administration and dose of SBEPC as well as to verify the neuroprotective effect of SBEPC on cerebral ischemia-reperfusion injury. RESULTS: The optimized preparation conditions of SBEPC were summarized as follows: the ratio of phospholipids to drug was 2:1, the drug concentration was 3.5 mg/ml, the reaction temperature was 50 °C, and the entrapment efficiency was over 93.00%. Stability studies have demonstrated that SBEPC should be stored under 40 °C in a dry and ventilated place away from light and below 37% humidity. Furthermore, pharmacodynamic studies have found that, compared with SBE, SBEPC could introduce drugs into the brain and better exert the neuroprotective effect on MCAO rats, and the optimal administration and dose concentration of SBEPC were nasal administration and 40 mg/ml, respectively. CONCLUSION: These findings demonstrate that SBEPC is successfully prepared by CCD-RSM. SBEPC can enhance drugs' ability to enter the brain and improve the bioavailability of drugs in brain, and can effectively exert the neuroprotective effect on cerebral ischemia-reperfusion injury as compared with SBE. Bentham Science Publishers 2022-02-25 2022-02-25 /pmc/articles/PMC9189737/ /pubmed/34376131 http://dx.doi.org/10.2174/1389201022666210729142257 Text en © 2022 Bentham Science Publishers https://creativecommons.org/licenses/by-nc/4.0/ This is an open access article licensed under the terms of the Creative Commons Attribution-Non-Commercial 4.0 International Public License (CC BY-NC 4.0) (https://creativecommons.org/licenses/by-nc/4.0/), which permits unrestricted, non-commercial use, distribution and reproduction in any medium, provided the work is properly cited.
spellingShingle Article
Chen, Shibin
Xie, Qiujie
Yang, Ming
Shi, Yajun
Shi, Junhui
Zeng, Xiaobin
Scutellaria baicalensis Extract-phospholipid Complex: Preparation and Initial Pharmacodynamics Research in Rats
title Scutellaria baicalensis Extract-phospholipid Complex: Preparation and Initial Pharmacodynamics Research in Rats
title_full Scutellaria baicalensis Extract-phospholipid Complex: Preparation and Initial Pharmacodynamics Research in Rats
title_fullStr Scutellaria baicalensis Extract-phospholipid Complex: Preparation and Initial Pharmacodynamics Research in Rats
title_full_unstemmed Scutellaria baicalensis Extract-phospholipid Complex: Preparation and Initial Pharmacodynamics Research in Rats
title_short Scutellaria baicalensis Extract-phospholipid Complex: Preparation and Initial Pharmacodynamics Research in Rats
title_sort scutellaria baicalensis extract-phospholipid complex: preparation and initial pharmacodynamics research in rats
topic Article
url https://www.ncbi.nlm.nih.gov/pmc/articles/PMC9189737/
https://www.ncbi.nlm.nih.gov/pubmed/34376131
http://dx.doi.org/10.2174/1389201022666210729142257
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