聚乙二醇-聚l -乳酸-硬脂酸逆负载阿司匹林胶束的构建及制备工艺优化

IF 1.8 4区 化学 Q3 POLYMER SCIENCE
Yunpeng Min, Hang Zhang, Huiru Wang, Yimin Song
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引用次数: 2

摘要

本工作旨在研究两亲性PEG-PLA-SA三嵌段共聚物反负载阿司匹林胶束的构建及制备工艺的优化。以聚乙二醇(PEG)为引发剂,采用l -丙交酯(L-LA)开环聚合法制备了PEG- pla二嵌段共聚物。以硬脂酸(SA)为原料,以4-二甲氨基吡啶(DMAP)和N,N'-双环己基碳二酰亚胺(DCC)为催化剂,与PEG-PLA反应制备最终产物PEG-PLA-SA三嵌段共聚物。利用傅里叶变换红外光谱仪(FT-IR)对产物结构进行表征。PEG-PLA-SA三嵌段共聚物在甲苯/乙醇/水体系中自组装形成反胶束,可将阿司匹林包裹成亲水性核。采用动态光散射(DLS)和透射电子显微镜(TEM)测定了反胶束的大小和形态。结果表明:反胶束呈球形,粒径小于70 nm;采用响应面分析法对PEG-PLA-SA的制备工艺进行优化。在37°C的磷酸盐缓冲盐水(PBS)中,在生物相容性膜中包埋反向负载阿司匹林胶束,实现体外药物释放。在前8 h,三嵌段共聚物的药物释放速度比二嵌段共聚物慢。8 h后,两种药物的释放速度趋于平缓。通过加速实验研究了阿司匹林反胶束的稳定性。这些结果表明,反胶束PEG-PLA-SA可能是一种很有前途的亲水药物载体,如阿司匹林。
本文章由计算机程序翻译,如有差异,请以英文原文为准。
Construction of poly(ethylene glycol)-poly(L-lactic acid)-stearic acid reverse aspirin-loaded micelles and optimization of preparation process.

This work aims to study the construction of reverse aspirin-loaded micelles prepared from amphiphilic PEG-PLA-SA triblock copolymers and the optimization of the preparation process. Using polyethylene glycol (PEG) as the initiator, ring-opening polymerization of L-lactide (L-LA) was used to prepare PEG-PLA diblock copolymers. Final product PEG-PLA-SA triblock copolymers were prepared by the reaction of stearic acid (SA) and PEG-PLA catalyzed by 4-dimethylaminopyridine (DMAP) and N,N'-Dicyclohexylcarbodiimide (DCC). Fourier transform infrared spectrometer (FT-IR) was used to characterize the product structure. PEG-PLA-SA triblock copolymers self-assembled in toluene/ethanol/water system to form reverse micelles, which could encapsulate aspirin into a hydrophilic core. Dynamic light scattering (DLS) and transmission electron microscopy (TEM) were used to determine the size and morphology of reverse micelles. The results showed that the reverse micelles are spherical, with a particle size of less than 70 nm. Response surface analysis method was applied to optimize the preparation process of PEG-PLA-SA. In vitro drug release was achieved by embedding reverse aspirin-loaded micelles in the biocompatible membrane in phosphate buffer saline (PBS) at 37°C. In the first 8 h, the drug release rate of the triblock copolymers was slower than that of the diblock copolymers. After 8 h, the drug release rate of both tended to be flat. The stability of aspirin-loaded reverse micelles was studied through accelerated test. These results indicate that reverse micelle PEG-PLA-SA may be a promising carrier for hydrophilic drugs like aspirin.

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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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