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聚氧乙烯-聚氧丙烯-聚氧乙烯三嵌段共聚物接枝肝素共聚物的合成与表征。

Synthesis and characterization of Poloxamer 188-grafted heparin copolymer.

机构信息

Pharmacy School, Wenzhou Medical College, Wenzhou, Zhejiang Province, PR China.

出版信息

Drug Dev Ind Pharm. 2010 Jul;36(7):832-8. doi: 10.3109/03639040903520983.

Abstract

BACKGROUND

Poloxamer 188 is a safe biocompatible polymer that can be used in protein drug delivery system.

AIM

In this study, a new heparin-poloxamer 188 conjugate (HP) was synthesized and its physicochemical properties were investigated. HP structure was confirmed by Fourier transform infrared spectroscopy (FTIR) and Hydrogen-1 nuclear magnetic resonance spectroscopy ((1)H-NMR). Content of the conjugated heparin was analyzed using Toluidine Blue. The critical micelle concentration (CMC) of the copolymer was determined by a fluorescence probe technique. The effect of HP on the gelation of poloxamer 188 was characterized by the rheological properties of the HP-poloxamer hydrogels. Solubility and viscosity of HP were also evaluated compared with poloxamer 188.

RESULTS

From the results, the solubility of the conjugated heparin was increased compared with free heparin. The content of heparin in HP copolymer was 62.9%. The CMC of HP and poloxamer 188 were 0.483 and 0.743 mg/mL, respectively. The gelation temperature of 0.4 g/mL HP was 43.5 degrees C, whereas that of the same concentration of poloxamer 188 was 37.3 degrees C. With HP content in poloxamer 188 solution increasing, a V-shape change of gelation temperature was observed.

CONCLUSION

Considering the importance of poloxamer 188 in functional material, HP may prove to be a facile temperature-sensitive material for protein drug-targeted therapy.

摘要

背景

泊洛沙姆 188 是一种安全的生物相容性聚合物,可用于蛋白质药物传递系统。

目的

本研究合成了一种新的肝素-泊洛沙姆 188 缀合物(HP),并对其理化性质进行了研究。通过傅里叶变换红外光谱(FTIR)和氢-1 核磁共振光谱(1H-NMR)证实了 HP 的结构。采用甲苯胺蓝法分析了缀合肝素的含量。采用荧光探针技术测定共聚物的临界胶束浓度(CMC)。通过 HP-泊洛沙姆 188 水凝胶的流变特性研究了 HP 对泊洛沙姆 188 凝胶化的影响。还与泊洛沙姆 188 比较了 HP 的溶解度和粘度。

结果

结果表明,与游离肝素相比,缀合肝素的溶解度增加。HP 共聚物中肝素的含量为 62.9%。HP 和泊洛沙姆 188 的 CMC 分别为 0.483 和 0.743mg/mL。浓度为 0.4g/mL 的 HP 的胶凝温度为 43.5℃,而相同浓度的泊洛沙姆 188 的胶凝温度为 37.3℃。随着 HP 在泊洛沙姆 188 溶液中的含量增加,胶凝温度呈 V 形变化。

结论

考虑到泊洛沙姆 188 在功能材料中的重要性,HP 可能被证明是一种用于蛋白质药物靶向治疗的简单的温度敏感材料。

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