PERMEABILITY STUDIES ON LIPOSOMES FORMED FROM POLYMERIZABLE DIACETYLENIC PHOSPHOLIPIDS AND THEIR POTENTIAL APPLICATIONS AS DRUG DELIVERY SYSTEMS
PERMEABILITY STUDIES ON LIPOSOMES FORMED FROM POLYMERIZABLE DIACETYLENIC PHOSPHOLIPIDS AND THEIR POTENTIAL APPLICATIONS AS DRUG DELIVERY SYSTEMS
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DOI：
10.1016/0304-4165(87)90032-8
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发表时间：
1987-05-19
期刊：
影响因子：
--
通讯作者：
CHAPMAN, D
中科院分区：
文献类型：
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作者：
FREEMAN, FJ;HAYWARD, JA;CHAPMAN, D
我们研究了由一组可聚合磷脂形成的脂质体的渗透性和包封特性，所述可聚合磷脂在其一个或两个酰基链中含有二炔基。通过释放包埋的染料6-羧基荧光素来评估渗透性。发现二炔磷脂酰胆碱（PC）脂质体表现出宽范围的渗透性，这取决于：（i）二炔脂质的性质，即，混合链（MC）或同链（ID），（ii）聚合程度，（iii）囊泡大小，和（iv）胆固醇含量。紫外线引发的聚合影响C25idPC脂质体的渗透性显着降低。聚合后由四种其他二炔类脂质（C25mcPC、C23idPC、C23mcPC和C20idPC）形成的脂质体的渗透性增加归因于脂质分子包装的干扰和/或小单层囊泡容纳长聚合物的能力有限。C20idPC脂质是非典型的，形成不规则的单体和聚合物囊泡。C25idPC脂质体的渗透性也通过[3H]菊粉的释放来评估。C25idPC脂质体在其单体和聚合状态下对[3H]菊粉表现出低渗透性。在人血浆中孵育C25idPC脂质体导致单体囊泡对羧基荧光素和[3H]菊粉的渗透性大幅增加。然而，在血浆存在下，聚合的C25idPC脂质体的渗透性不受影响，50 h后囊泡保留了大部分截留的[3H]菊粉。这些发现表明，聚合物C25idPC脂质体表现出对血浆组分如高密度脂蛋白（HDL）的破坏作用的高抗性。聚合物C25idPC脂质体可能在药物递送系统中具有应用。
We have investigated the permeability and entrapment characteristics of liposomes formed from a group of polymerisable phospholipids, containing diacetylenic groups in one or both of their acyl chains. Permeability was assessed by the release of an entrapped dye, 6-carboxyfluorescein. Diacetylenic phosphatidylcholine (PC) liposomes were found to exhibit a wide range of permeability properties, depending on: (i) the nature of the diacetylenic lipid, i.e., mixed-chain (mc) or identical-chain (id), (ii) the extent of polymerisation, (iii) vesicle size, and (iv) cholesterol content. Ultraviolet-initiated polymerisation affected a significant decrease in the permeability of C25idPC liposomes. The increase in permeability of liposomes formed from four other diacetylenic lipids (C25mcPC, C23idPC,C23mcPC and C20idPC) after polymerisation was attributed to disturbances in the packing of lipid molecules, and/or the limited ability of small unilamellar vesicles to accommodate long polymers. The C20idPC lipid is atypical, forming irregular monomeric and polymeric vesicles. The permeability of C25idPC liposomes was also assessed by the release of [3H]inulin. C25idPC liposomes exhibited low permeabilities to [3H]inulin in their monomeric and polymeric states. Incubation of C25idPC liposomes in human plasma caused a substantial increase in the permeability of monomeric vesicles to both carboxyfluorescein and [3H]inulin. The permeability of polymerised C25idPC liposomes, however, was unaffected in the presence of plasma, with vesicles retaining most of their entrapped [3H]inulin after 50 h. These findings demonstrate that polymeric C25idPC liposomes exhibit high resistance to the destructive actions of plasma components, such as high-density lipoproteins (HDLs). Polymeric C25idPC liposomes may have an application in drug delivery systems.