新型材料胆固醇聚乙二醇氨基CLS-PEG-NH2修饰药物及缓释药物研发方向

胆固醇-聚乙二醇-胺基CLS-PEG-NH2/CHOL-PEG-NH2利用非常稳定的化学键,通过醚键或酰胺键将胆固醇和胺连接到聚乙二醇上。与在水溶液中容易水解的酯键不同,胆固醇和PEG之间的醚键具有化学稳定性。胆固醇是一种膜成分,具有调节膜流动性、弹性和渗透性的功能。当蛋白质嵌入膜中时,它填补了其他脂质物种堆积形成的空隙。为华生物胆固醇聚乙二醇氨基CLS-PEG-NH2的应用:CLS-PEG-NH2(胆固醇聚乙二醇胺)是一种具有良好水溶性的亲脂性脂质PEG缀合物。PEG胆固醇衍生物可用于制备脂质体以改善包封药物的循环时间,它们也可用于非病毒转染试剂。聚乙二醇化胆固醇作为一种两亲性脂质衍生物,可用于制备脂质体和其他胶束作为药物传递系统,用于药物修饰或缓释药物研发,新型材料探究。
用水溶性单甲氧基聚乙二醇2000 (mPEG2000)通过小分子的胺与胆固醇连接,制备mPEG2000修饰的胆固醇衍生物。该衍生物可以作为多种制剂的辅料,如作为表面活性剂用来制备水溶液分散体:纳米乳剂,纳米脂质体;也可以作为载体成分之一用来制备能分散于水的胶束、固体脂质纳米粒;还可以作为长循环纳米、温度或pH敏感性纳米载体的成分之一。
注意事项:CLS-PEG-NH2(胆固醇聚乙二醇胺)材料易吸潮,取用前需放置室温后再打开包装取用防止吸潮,吸潮后活性会降低直至完全失去活性,请务必保持干燥,同时尽量避免频繁的溶解和冻干。

Cholesterol polyethylene glycol amine cls-peg-nh2 / chol-peg-nh2 uses very stable chemical bonds to connect cholesterol and amine to polyethylene glycol through ether or amide bonds. Unlike the ester bond that is easily hydrolyzed in aqueous solution, the ether bond between cholesterol and peg is chemically stable. Cholesterol is a membrane component with the function of regulating membrane fluidity, elasticity and permeability. When the protein is embedded in the membrane, it fills the gap formed by the accumulation of other lipid species. Application of cholesterol polyethylene glycol amino cls-peg-nh2 of Weihua biology: cls-peg-nh2 (cholesterol polyethylene glycol amine) is a lipophilic lipid peg conjugate with good water solubility. Peg cholesterol derivatives can be used to prepare liposomes to improve the circulation time of encapsulated drugs, and they can also be used as non viral transfection reagents. As an amphiphilic lipid derivative, pegylated cholesterol can be used to prepare liposomes and other micelles as drug delivery systems, for drug modification or sustained-release drug development, and for new material exploration.
Water soluble monomethoxy polyethylene glycol 2000 (mpeg2000) was linked to cholesterol through small molecule amine to prepare mpeg2000 modified cholesterol derivatives. The derivatives can be used as excipients of various preparations, such as surfactants to prepare aqueous dispersion: nano emulsions, nano liposomes; It can also be used as one of the carrier components to prepare micelles and solid lipid nanoparticles that can be dispersed in water; It can also be used as one of the components of long cycle nano, temperature or pH sensitive nanocarriers.
Precautions: cls-peg-nh2 (cholesterol polyethylene glycol amine) material is easy to absorb moisture. Before taking it, it needs to be placed at room temperature before opening the package to prevent moisture absorption. After moisture absorption, the activity will decrease until it completely loses its activity. Please keep it dry and try to avoid frequent dissolution and lyophilization.
