Alkan-Onyuksel H, Son K
Department of Pharmaceutics, University of Illinois, College of Pharmacy, Chicago 60612.
Pharm Res. 1992 Dec;9(12):1556-62. doi: 10.1023/a:1015804206414.
The aqueous solubility of teniposide in detergent and phospholipid mixed micelles was investigated as functions of the detergents and lipids composing the mixed micelles, the molar ratio of detergent to phospholipid, and the total lipid concentration of the system. The polarity, the charge of the phospholipid, and its saturation affected the solubilization potential of the micelles. Physical chemical factors such as the pH, ionic strength, and temperature of the dispersion medium also altered the solubilization capacity of the system. The results are explained by the changes occurring in the critical micelle concentration and packing arrangements of the aggregates. The desired solubility of teniposide can be achieved by adjusting the studied parameters to the optimum values. Teniposide-containing mixed micelles were spontaneously converted to drug-containing vesicles upon aqueous dilution; therefore, the precipitation of the drug was totally eliminated. In conclusion, mixed micelles as proliposomes can be a suitable drug carrier system for insoluble compounds such as teniposide.
研究了替尼泊苷在去污剂和磷脂混合胶束中的水溶性,考察了组成混合胶束的去污剂和脂质、去污剂与磷脂的摩尔比以及体系总脂质浓度对其的影响。磷脂的极性、电荷及其饱和度影响胶束的增溶潜力。分散介质的pH、离子强度和温度等物理化学因素也会改变体系的增溶能力。这些结果可通过聚集体临界胶束浓度和堆积排列的变化来解释。通过将研究参数调整到最佳值,可以实现替尼泊苷所需的溶解度。含替尼泊苷的混合胶束在水稀释后会自发转化为含药囊泡;因此,药物的沉淀被完全消除。总之,作为前体脂质体的混合胶束可以成为替尼泊苷等不溶性化合物的合适药物载体系统。