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SYNTHESIS AND LIPOSOMES OF A NOVEL KIND OF AMPHIPHILIC AMINO ACID

机译:新型两亲性氨基酸的合成与脂质体

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Polymerized liposomes have been studied in recent years as stable biomembrane model and drug delivery system. Among these liposomes, the amphiphiles having unsaturated carbon-carbon bonds, such as diyne or diene can be polymerized by UV irradiation and result in the stabilization of the self-assemblied structures while preserving their morphological features. However, the resulting polyolfins after addition polymerization are difficult to degrade in vivo, and sometimes even cause toxic, which greatly limit their uses as drug carriers. Condensable liposomes from amphiphilic amino acids as potential biodegradable drug carriers, can form a polypeptide net on their surface through condensation polymerization, which may increase their biocompability and half life time in vivo. In this paper, a novel kind of amphiphilic amino acid S-[l-carboxy-2-([N-(l,2-bisoctadecyloxycarbonyl )ethyl] carbanoyl ) ethyl] cysteine (Asp18-M-Cys) was synthesized and the formation of stable liposome was confirmed. It can be polymerized in lipid bilayer membrane and change the stability and permeability of the liposomes .
机译:近年来,已经研究了聚合脂质体作为稳定的生物膜模型和药物递送系统。在这些脂质体中,具有不饱和碳-碳键的两亲物,例如二炔或二烯,可以通过紫外线照射而聚合,并在保持其形态特征的同时使自组装结构稳定。然而,加成聚合后所得的多元醇在体内难以降解,有时甚至引起毒性,这极大地限制了其作为药物载体的用途。来自两亲氨基酸的可凝缩脂质体作为潜在的可生物降解的药物载体,可通过缩聚作用在其表面形成多肽网,这可增加其生物相容性和体内半衰期。本文合成了一种新型的两亲性氨基酸S- [1-羧基-2-([N-(1,2-双十八烷基氧羰基)乙基]氨基甲酰基)乙基]半胱氨酸(Asp18-M-Cys)确认了稳定的脂质体。它可以在脂质双层膜中聚合并改变脂质体的稳定性和通透性。

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