首页> 外国专利> PROCESS FOR PREPARING NANOCARRIERS TO BE USED FOR VECTORIZATION OF INTERFERENCE RIBONUCLEIC ACID () AND TARGETED DELIVERY TO AORTIC VALVE CELLS

PROCESS FOR PREPARING NANOCARRIERS TO BE USED FOR VECTORIZATION OF INTERFERENCE RIBONUCLEIC ACID () AND TARGETED DELIVERY TO AORTIC VALVE CELLS

机译:制备用于干扰核糖核酸()的靶向和靶向输送至主动脉瓣细胞的纳米载体的方法

摘要

The invention relates to a process for preparing nano-bio-particles to be used for targeted delivery of nucleic acids to the cells of a malfunctioning aortic valve. According to the invention, the process consists in combining the main components, namely 50% M a positively charged phospholipid such as 1,2-dioleoyl-3-trimethylammonium-propane (DOTAP) with 35% M a neutral pH-sensitive phospholipid, such as 1,2-dioleoyl-sn-glycero-3-phosphoethanol amine (DOPE), 1...14% M palmitoyl homocysteine (PHC) and 1% M a phospholipide derivative of polyethylene glycol functionalized with maleimide (Mal-PEG-DSPE), the mixture is dissolved in chloroform, as such or in admixture with methanol in a ratio of 9:1, the lipid film is hydrated up to a concentration of 10 mM, followed by the suspension extrusion, to result in PEGylated cathionic liposomes having characteristics of membrane anchor for specific ligand binding, in view of targeted delivery to malfunctioning aortic valve.
机译:本发明涉及一种制备纳米生物粒子的方法,该纳米生物粒子用于将核酸靶向递送至失灵的主动脉瓣细胞。根据本发明,该方法包括将主要成分,即50%M的带正电的磷脂如1,2-二油酰基-3-三甲基铵-丙烷(DOTAP)与35%M的中性pH敏感的磷脂,例如作为1,2-二油酰基-sn-甘油-3-磷酸乙醇胺(DOPE),1 ... 14%M棕榈酰基高半胱氨酸(PHC)和1%M是经马来酰亚胺官能化的聚乙二醇的磷脂衍生物(Mal-PEG-DSPE ),将混合物原样溶解在氯仿中或与甲醇以9:1的比例混合,将脂质膜水合至浓度为10 mM,然后将悬浮液挤出,得到具有以下成分的聚乙二醇化阳离子脂质体考虑到向主动脉瓣的靶向递送,针对特定配体结合的膜锚的特性。

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