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Fabrication of triblock ABA type peptide dendrimer based on glutamic acid dimethyl ester and PEG as a potential nano drug delivery agent

机译:基于谷氨酸二甲酯和PEG作为潜在的纳米药物递送剂的三嵌段ABA型肽树状聚合物的制备

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Introduction Peptide dendrimers build up from amino acids and they simulate to artificial proteins with globular architecture. These characteristics furnish dendrimers with best biodegradability and biocompatibility in drug delivery systems. Methods A barbell-like dendrimer from glutamic acid dimethyl ester-poly (ethylene glycol)-glutamic acid dimethyl ester as ABA-type triblock copolymer PG-PEG-PG) was prepared with liquid-phase peptide synthesis via a divergent approach. PEG 600 diacid (PEG-A) and glutamic acid dimethyl ester were as the core and the monomeric building blocks, respectively. Linear-dendritic copolymer was prepared in the presence of DCC in pyridine. Transmission electron microscope (TEM) was used for measuring the size of first generation (G1-COOH) and second generation (G2-COOH) of dendrimer compounds. Thermal behavior of the synthesized dendrimers was investigated using DSC. Results The desired generations G1-COOH, G2-COOH and G3-COOH were prepared by divergent method using PEG diacid 600 as a core compound. The size range of the resulted particles was found to be 20-100 nm for various generations. The isolated dendrimer was examined as the drug-delivery agent and the controlled release was carried out for drug molecule in pH 7.4. Conclusion Based on the obtained results, the synthesized biocompatible dendrimers could potentially be utilized as a drug carrier agent.
机译:简介肽树状大分子由氨基酸组成,它们模拟为具有球形结构的人工蛋白质。这些特性使树状聚合物在药物递送系统中具有最佳的生物降解性和生物相容性。方法以液相肽合成为原料,通过谷氨酸二甲酯-聚(乙二醇)-谷氨酸二甲酯为ABA型三嵌段共聚物PG-PEG-PG)制备杠铃状树枝状大分子。 PEG 600二酸(PEG-A)和谷氨酸二甲酯分别为核心和单体结构单元。在吡啶中在DCC存在下制备线性-树状共聚物。透射电子显微镜(TEM)用于测量第一代(G1-COOH)和第二代(G2-COOH)树枝状化合物的尺寸。使用DSC研究了合成的树枝状大分子的热行为。结果以PEG二酸600为核心化合物,采用发散法制备了所需的G1-COOH,G2-COOH和G3-COOH。对于各种世代,发现所得颗粒的尺寸范围为20-100nm。检查分离的树枝状大分子作为药物递送剂,并在pH 7.4下对药物分子进行控释。结论根据获得的结果,合成的生物相容性树状聚合物可潜在地用作药物载体。

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