Preparation and in vitro release of total alkaloids from alstonia scholaris leaf-loaded mPEG-PMA microspheres

The total alkaloids extracted from the leaves of Alstonia scholaris (ASAs) have been reported to reduce fever, remove phlegm, and relieve coughs. However, their drug half-lives are short. Thus, to obtain sustained-release preparations of total alkaloids from ASAs, mandelic acid oxyanhydride (mandeli...

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Main Authors: Nianfeng Jiang, Xiangyu Zheng, Yan Feng, Hongtao Wu, Mingwei Yuan, Yi He, Hongli Li, Minglong Yuan
Format: Article
Language:English
Published: IOP Publishing 2021-01-01
Series:Materials Research Express
Subjects:
Online Access:https://doi.org/10.1088/2053-1591/ac1cab
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author Nianfeng Jiang
Xiangyu Zheng
Yan Feng
Hongtao Wu
Mingwei Yuan
Yi He
Hongli Li
Minglong Yuan
author_facet Nianfeng Jiang
Xiangyu Zheng
Yan Feng
Hongtao Wu
Mingwei Yuan
Yi He
Hongli Li
Minglong Yuan
author_sort Nianfeng Jiang
collection DOAJ
description The total alkaloids extracted from the leaves of Alstonia scholaris (ASAs) have been reported to reduce fever, remove phlegm, and relieve coughs. However, their drug half-lives are short. Thus, to obtain sustained-release preparations of total alkaloids from ASAs, mandelic acid oxyanhydride (mandelic acid OCA) was synthesized by the reaction of L-mandelic acid (MA) with triphosgene, and subsequent copolymerization with polyethylene glycol monomethyl ether (mPEG) of different molecular weights yielded the corresponding mPEG poly-MA (mPEG-PMA) copolymers. ASAs-loaded microspheres were then prepared using the double emulsion method, and their in vitro release (15 d, 37 °C) and in vitro degradation behaviors were studied. The morphology, size, embedding efficiency, and drug loading efficiency were investigated for the prepared microspheres, and screening was carried out using the mPEG _10K -PMA drug-loaded microspheres to analyze their biological characteristics. Anti-inflammatory experiments using Kunming mice and Sprague Dawley rats showed that the microspheres exhibited good anti-inflammatory properties. Moreover, the ASAs-loaded microspheres exhibited a good biocompatibility, and the hemolysis rate was <5%.
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spelling doaj.art-ae7539eec8d041f7b069fe90212bfe012023-08-09T15:52:53ZengIOP PublishingMaterials Research Express2053-15912021-01-018808530410.1088/2053-1591/ac1cabPreparation and in vitro release of total alkaloids from alstonia scholaris leaf-loaded mPEG-PMA microspheresNianfeng Jiang0Xiangyu Zheng1Yan Feng2Hongtao Wu3Mingwei Yuan4Yi He5Hongli Li6https://orcid.org/0000-0002-8303-8615Minglong Yuan7National and Local Joint Engineering Research Center for Green Preparation Technology of Biobased Materials, Yunnan Minzu University , Kunming 650500, People’s Republic of ChinaJilin Institute of Chemical Technology, Jilin 132000, People’s Republic of ChinaNational and Local Joint Engineering Research Center for Green Preparation Technology of Biobased Materials, Yunnan Minzu University , Kunming 650500, People’s Republic of ChinaNational and Local Joint Engineering Research Center for Green Preparation Technology of Biobased Materials, Yunnan Minzu University , Kunming 650500, People’s Republic of ChinaNational and Local Joint Engineering Research Center for Green Preparation Technology of Biobased Materials, Yunnan Minzu University , Kunming 650500, People’s Republic of ChinaSchool of Chemistry and Chemical Engineering, and Chongqing Key Laboratory of Soft-Matter Material Chemistry and Functional Manufacturing, Southwest University , Chongqing 400715, People’s Republic of ChinaNational and Local Joint Engineering Research Center for Green Preparation Technology of Biobased Materials, Yunnan Minzu University , Kunming 650500, People’s Republic of ChinaNational and Local Joint Engineering Research Center for Green Preparation Technology of Biobased Materials, Yunnan Minzu University , Kunming 650500, People’s Republic of ChinaThe total alkaloids extracted from the leaves of Alstonia scholaris (ASAs) have been reported to reduce fever, remove phlegm, and relieve coughs. However, their drug half-lives are short. Thus, to obtain sustained-release preparations of total alkaloids from ASAs, mandelic acid oxyanhydride (mandelic acid OCA) was synthesized by the reaction of L-mandelic acid (MA) with triphosgene, and subsequent copolymerization with polyethylene glycol monomethyl ether (mPEG) of different molecular weights yielded the corresponding mPEG poly-MA (mPEG-PMA) copolymers. ASAs-loaded microspheres were then prepared using the double emulsion method, and their in vitro release (15 d, 37 °C) and in vitro degradation behaviors were studied. The morphology, size, embedding efficiency, and drug loading efficiency were investigated for the prepared microspheres, and screening was carried out using the mPEG _10K -PMA drug-loaded microspheres to analyze their biological characteristics. Anti-inflammatory experiments using Kunming mice and Sprague Dawley rats showed that the microspheres exhibited good anti-inflammatory properties. Moreover, the ASAs-loaded microspheres exhibited a good biocompatibility, and the hemolysis rate was <5%.https://doi.org/10.1088/2053-1591/ac1cabdrug loadingbiocompatibilityanti-inflammatory livenesshemolysis rate
spellingShingle Nianfeng Jiang
Xiangyu Zheng
Yan Feng
Hongtao Wu
Mingwei Yuan
Yi He
Hongli Li
Minglong Yuan
Preparation and in vitro release of total alkaloids from alstonia scholaris leaf-loaded mPEG-PMA microspheres
Materials Research Express
drug loading
biocompatibility
anti-inflammatory liveness
hemolysis rate
title Preparation and in vitro release of total alkaloids from alstonia scholaris leaf-loaded mPEG-PMA microspheres
title_full Preparation and in vitro release of total alkaloids from alstonia scholaris leaf-loaded mPEG-PMA microspheres
title_fullStr Preparation and in vitro release of total alkaloids from alstonia scholaris leaf-loaded mPEG-PMA microspheres
title_full_unstemmed Preparation and in vitro release of total alkaloids from alstonia scholaris leaf-loaded mPEG-PMA microspheres
title_short Preparation and in vitro release of total alkaloids from alstonia scholaris leaf-loaded mPEG-PMA microspheres
title_sort preparation and in vitro release of total alkaloids from alstonia scholaris leaf loaded mpeg pma microspheres
topic drug loading
biocompatibility
anti-inflammatory liveness
hemolysis rate
url https://doi.org/10.1088/2053-1591/ac1cab
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