Amphoteric liposomes, method of formulating an amphoteric liposome and a method of loading an amphoteric liposome
申请人:novosom AG
公开号:EP1911443A1
公开(公告)日:2008-04-16
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,由脂质混合物组成,所述混合物包括阳离子两性化合物、阴离子两性化合物和一种或多种中性两性化合物、所述阳离子和阴离子双亲化合物中至少有一种是可带电的,且阳离子和阴离子双亲化合物各自的量应选择为:在第一个较低的 pH 值下,带正电的阳离子双亲化合物按比例过量,在第二个较高的 pH 值下,带负电的阴离子双亲化合物按比例过量,且所述混合物的等电点介于所述第一和第二 pH 值之间;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化合物可在所述等电点相互形成脂盐。还公开了预测两性脂质体在给定 pH 值下的溶融性、配制两性脂质体和用货物分子装载两性脂质体的方法。