Amphoteric Liposomes, A Method Of Formulating An Amphoteric Liposome And A Method Of Loading An Amphoteric Liposome
申请人:Panzner Steffen
公开号:US20120135065A1
公开(公告)日:2012-05-31
An amphoteric liposome composed of a mixture of lipids, said mixture comprising a cationic amphiphile, an anionic amphiphile and optionally one or more neutral amphiphiles, at least one of said cationic and anionic amphiphiles being chargeable and the respective amounts of said cationic and anionic amphiphiles being selected such there is a stoichiometric excess of positively charged cationic amphiphile at a first lower pH, a stoichiometric excess of negatively charged anionic amphiphile at a second higher pH and said mixture has an isoelectric point intermediate said first and second pHs; characterised in that said positively charged cationic and negatively charged anionic amphiphiles are adapted to form a lipid salt with one another at said isoelectric point. Also disclosed are methods of predicting the fusogenicity of an amphoteric liposome at a given pH, formulating an amphoteric liposome and loading an amphoteric liposome with a cargo moiety.
一种两性脂质体,由混合脂质组成,所述混合物包括阳离子两性分子、阴离子两性分子和可选的一个或多个中性两性分子,其中至少一种阳离子和阴离子两性分子是可带电的,并且所述阳离子和阴离子两性分子的相应量被选择为在第一个较低的pH值下存在过量的带正电荷的阳离子两性分子,在第二个较高的pH值下存在过量的带负电荷的阴离子两性分子,并且所述混合物具有介于第一个和第二个pH值之间的等电点;其特征在于所述带正电荷的阳离子和带负电荷的阴离子两性分子被适应在所述等电点处彼此形成脂质盐。还公开了预测在给定pH下两性脂质体的融合性、制备两性脂质体和将载荷基团装载到两性脂质体中的方法。