Son K, Alkan H
Department of Pharmaceutics, College of Pharmacy, University of Illinois, Chicago 60612.
Biochim Biophys Acta. 1989 Jun 6;981(2):288-94. doi: 10.1016/0005-2736(89)90039-4.
Quasi-elastic light scattering (QELS) studies showed that vesicles can spontaneously form from sodium glycocholate-egg phosphatidylcholine mixed micelles upon dilution with physiological saline buffer (pH 7.5). A water-soluble drug, cytosine arabinoside, did not affect the transition pattern. Transitions were also obtained when dilutions were performed using diluted serum solutions (5% and 10% serum in buffer). However, if intermicellar bile salt monomer concentration (imc) was kept constant in diluent media, the transition was completely suppressed. Approximately 10% of the cytosine arabinoside was trapped inside vesicles which were formed in buffer, although this value decreased to approx. 2.5% when diluted serum was used. These results suggest that the mixed micelle to vesicle transition can be an alternative means to sonication in loading drugs into in vitro vesicles. A good correlation was found between the transmission electron microscopy (TEM) diameter and the mean hydrodynamic diameter obtained by QELS.
准弹性光散射(QELS)研究表明,用生理盐缓冲液(pH 7.5)稀释时,甘氨胆酸钠 - 卵磷脂混合胶束可自发形成囊泡。水溶性药物阿糖胞苷不影响转变模式。用稀释血清溶液(缓冲液中5%和10%血清)进行稀释时也能得到转变。然而,如果稀释介质中胶束间胆汁盐单体浓度(imc)保持恒定,则转变被完全抑制。约10%的阿糖胞苷被困在缓冲液中形成的囊泡内,不过当使用稀释血清时,该值降至约2.5%。这些结果表明,混合胶束到囊泡的转变可能是一种替代超声处理将药物载入体外囊泡的方法。透射电子显微镜(TEM)直径与QELS获得的平均流体动力学直径之间存在良好的相关性。