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在不同pH值下获得的聚[(2-二甲基氨基)乙基甲基丙烯酸酯]/硫酸软骨素聚电解质复合物:I. 硫酸软骨素的制备、表征、细胞毒性和控释

Polyelectrolyte complexes of poly[(2-dimethylamino) ethyl methacrylate]/chondroitin sulfate obtained at different pHs: I. Preparation, characterization, cytotoxicity and controlled release of chondroitin sulfate.

作者信息

Bonkovoski Letícia C, Martins Alessandro F, Bellettini Ismael C, Garcia Francielle P, Nakamura Celso V, Rubira Adley F, Muniz Edvani C

机构信息

Grupo de Materiais Poliméricos e Compósitos, Departamento de Química, Universidade Estadual de Maringá UEM, Av. Colombo 5790, 87020-900 Maringá, PR, Brazil.

Grupo de Materiais Poliméricos e Compósitos, Departamento de Química, Universidade Estadual de Maringá UEM, Av. Colombo 5790, 87020-900 Maringá, PR, Brazil; Universidade Tecnológica Federal do Paraná (UTFPR), Estrada para Boa Esperança, 85660-000 Dois Vizinhos, PR, Brazil.

出版信息

Int J Pharm. 2014 Dec 30;477(1-2):197-207. doi: 10.1016/j.ijpharm.2014.10.017. Epub 2014 Oct 12.

DOI:10.1016/j.ijpharm.2014.10.017
PMID:25311176
Abstract

For the first time, polyelectrolyte complex based on poly[(2-dimethylamino) ethyl methacrylate] (PDMAEMA) and chondroitin sulfate (CS) was prepared. The properties of novel material and precursors were investigated by WAXS, FTIR, TGA, SEM and DLS analysis. The PDMAEMA/CS PECs presented hydrophilic-hydrophobic transition at pHs 6.0, 7.0 and 8.0 whereas the non-complexed PDMAEMA showed such a transition at pH 8.0 and not at pHs 6.0 and 7.0. Studies of CS release from PECs at pHs 6 and 8 confirmed that the samples possess the potential to release the CS in alkaline and not in acidic conditions. Since PECs are thermo-responsive due to the reduction of LCST caused by the increase in pH, the release of CS was dependent on temperature and pH factors. Cytotoxicity assays using healthy VERO cells showed that the complexation between CS and PDMAEMA increased the PECs' biocompatibility related to PDMAEMA. However, the biocompatibility depends on the amount of CS present in the PECs.

摘要

首次制备了基于聚甲基丙烯酸(2-二甲氨基)乙酯(PDMAEMA)和硫酸软骨素(CS)的聚电解质复合物。通过广角X射线散射(WAXS)、傅里叶变换红外光谱(FTIR)、热重分析(TGA)、扫描电子显微镜(SEM)和动态光散射(DLS)分析研究了这种新型材料及其前体的性能。PDMAEMA/CS聚电解质复合物在pH值为6.0、7.0和8.0时呈现亲水-疏水转变,而非复合的PDMAEMA仅在pH值为8.0时呈现这种转变,在pH值为6.0和7.0时则没有。对聚电解质复合物在pH值为6和8时CS释放情况的研究证实,这些样品具有在碱性而非酸性条件下释放CS的潜力。由于聚电解质复合物因pH值升高导致最低临界溶液温度(LCST)降低而具有热响应性,CS的释放取决于温度和pH值因素。使用健康的非洲绿猴肾细胞(VERO细胞)进行的细胞毒性试验表明,CS与PDMAEMA之间的络合作用提高了聚电解质复合物相对于PDMAEMA的生物相容性。然而,生物相容性取决于聚电解质复合物中CS的含量。

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