Preparation and in vivo/in vitro characterization of Ticagrelor PLGA sustained-release microspheres for injection.

IF 1.8 4区 化学 Q3 POLYMER SCIENCE
Designed Monomers and Polymers Pub Date : 2021-10-08 eCollection Date: 2021-01-01 DOI:10.1080/15685551.2021.1984008
Linkun Hao, Yunying Jiang, Ru Zhang, Ningning Zhang, Yang Yang, Ying Gao, Yimin Song
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引用次数: 2

Abstract

The objective of this paper was to develop a PLGA carrier Ticagrelor sustained-release microspheres preparation, which was expected to continue to release Ticagrelor for 14 days with a high encapsulation rate. Ticagrelor microspheres were prepared successfully with average diameter of 7.31 µm, drug loading of 12.49 ± 0.32% and EE up to 79.09 ± 1.69%. In the release medium of PH7.4 PBS, the microspheres showed good drug release behavior in vitro. In vivo release results also showed that the sustained-release microspheres could effectively control drug release in vivo and maintain a relatively stable blood drug concentration for about 2 weeks. The results indicate that Ticagrelor sustained-release microspheres can be used for long-term treatment of acute coronary syndrome.

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注射用替格瑞洛PLGA缓释微球的制备及体内外表征。
本文的目的是开发一种PLGA载体替格瑞洛缓释微球制剂,该制剂有望以高包封率持续释放替格瑞洛14天。成功制备了替格瑞洛微球,平均直径为7.31µm,载药量为12.49±0.32%,EE高达79.09±1.69%。在PH7.4 PBS释放介质中,微球表现出良好的体外释药行为。体内释放结果也表明,缓释微球能有效控制体内药物释放,维持相对稳定的血药浓度约2周。结果表明替格瑞洛缓释微球可用于急性冠脉综合征的长期治疗。
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来源期刊
Designed Monomers and Polymers
Designed Monomers and Polymers 化学-高分子科学
CiteScore
3.30
自引率
0.00%
发文量
28
审稿时长
2.1 months
期刊介绍: Designed Monomers and Polymers ( DMP) publishes prompt peer-reviewed papers and short topical reviews on all areas of macromolecular design and applications. Emphasis is placed on the preparations of new monomers, including characterization and applications. Experiments should be presented in sufficient detail (including specific observations, precautionary notes, use of new materials, techniques, and their possible problems) that they could be reproduced by any researcher wishing to repeat the work. The journal also includes macromolecular design of polymeric materials (such as polymeric biomaterials, biomedical polymers, etc.) with medical applications. DMP provides an interface between organic and polymer chemistries and aims to bridge the gap between monomer synthesis and the design of new polymers. Submssions are invited in the areas including, but not limited to: -macromolecular science, initiators, macroinitiators for macromolecular design -kinetics, mechanism and modelling aspects of polymerization -new methods of synthesis of known monomers -new monomers (must show evidence for polymerization, e.g. polycondensation, sequential combination, oxidative coupling, radiation, plasma polymerization) -functional prepolymers of various architectures such as hyperbranched polymers, telechelic polymers, macromonomers, or dendrimers -new polymeric materials with biomedical applications
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