LIPOSOMES OBTAINED BY THE ETHANOL INJECTION METHOD

LIPOSOMES OBTAINED BY THE ETHANOL INJECTION METHOD
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DOI:
10.1016/0378-5173(93)90389-w
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发表时间:
1993-06-30
影响因子:
5.8
通讯作者:
ESTELRICH, J
ESTELRICH, J
中科院分区:
医学2区
文献类型:
--
作者:
PONS, M;FORADADA, M;ESTELRICH, J

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获得脂质体最简单的方法之一是所谓的乙醇注射。这是一个温和的过程,提供了一个相当均匀的水泡数量,尽管相当稀释。考察了脂类浓度、渗透压和介质pH值对脂质体粒径分布的影响。另一方面,为了建立包封率与化学特性之间的关系,对8种物质进行了包埋。结果表明,40 mg/ml的脂质浓度会产生平均直径小于100 nm的囊泡,这一群体是最均匀的。渗透压和pH的影响不是很重要。在药物包封率方面,溶解在与脂质相同的乙醇中的药物包封率相对较好,而亲水性物质如羧基荧光素的包封率较低。其他种类的药物,如喹诺酮类、环丙沙星和恩诺沙星,包封率较高,但最终产率较低。
One of the most simple methods of obtaining liposomes is the so-called ethanol injection. This is a mild procedure which affords a reasonably homogeneous vesicle population, although rather diluted. We have observed the influence of lipid concentration, osmolality and pH of medium on the size distribution of liposomes. On the other hand, eight substances have been encapsulated in order to establish the relation between efficiency of encapsulation and chemical characteristics. Results obtained show that a 40 mg/ml lipid concentration produces vesicles below 100 nm average diameter, this population being the most homogeneous. The effect of osmolality and pH is less important. With respect to drug encapsulation, drugs dissolved in the same ethanol as the lipid are relatively well encapsulated, whereas hydrophilic substances such as carboxyfluorescein show lower entrapment. Other kinds of drugs like the quinolones cyprofloxacin and enrofloxacin are associated with high encapsulation efficiencies but the final yield is low.