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...
Main Authors: | , , , , , , , |
---|---|
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 |
_version_ | 1797746899008094208 |
---|---|
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%. |
first_indexed | 2024-03-12T15:43:23Z |
format | Article |
id | doaj.art-ae7539eec8d041f7b069fe90212bfe01 |
institution | Directory Open Access Journal |
issn | 2053-1591 |
language | English |
last_indexed | 2024-03-12T15:43:23Z |
publishDate | 2021-01-01 |
publisher | IOP Publishing |
record_format | Article |
series | Materials Research Express |
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 |
work_keys_str_mv | AT nianfengjiang preparationandinvitroreleaseoftotalalkaloidsfromalstoniascholarisleafloadedmpegpmamicrospheres AT xiangyuzheng preparationandinvitroreleaseoftotalalkaloidsfromalstoniascholarisleafloadedmpegpmamicrospheres AT yanfeng preparationandinvitroreleaseoftotalalkaloidsfromalstoniascholarisleafloadedmpegpmamicrospheres AT hongtaowu preparationandinvitroreleaseoftotalalkaloidsfromalstoniascholarisleafloadedmpegpmamicrospheres AT mingweiyuan preparationandinvitroreleaseoftotalalkaloidsfromalstoniascholarisleafloadedmpegpmamicrospheres AT yihe preparationandinvitroreleaseoftotalalkaloidsfromalstoniascholarisleafloadedmpegpmamicrospheres AT honglili preparationandinvitroreleaseoftotalalkaloidsfromalstoniascholarisleafloadedmpegpmamicrospheres AT minglongyuan preparationandinvitroreleaseoftotalalkaloidsfromalstoniascholarisleafloadedmpegpmamicrospheres |