MIXED MICELLES AS PROLIPOSOMES FOR THE SOLUBILIZATION OF TENIPOSIDE

被引:40
作者
ALKANONYUKSEL, H
SON, K
机构
[1] Department of Pharmaceutics, University of Illinois at Chicago, College of Pharmacy, Chicago, Illinois
[2] Daewoong Pharmaceutical Co. Ltd., Sungnam City
关键词
TENIPOSIDE; MIXED MICELLES; BILE SALTS; PHOSPHOLIPIDS; LIPOSOMES; SOLUBILIZATION; SERUM PROTEINS;
D O I
10.1023/A:1015804206414
中图分类号
O6 [化学];
学科分类号
0703 ;
摘要
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.
引用
收藏
页码:1556 / 1562
页数:7
相关论文
共 25 条
[1]  
[Anonymous], 1990, LIPOSOMES PRACTICAL
[2]  
Attwood D, 1983, SURFACTANT SYSTEMS
[3]   INTERACTIONS OF THE LOCAL-ANESTHETIC TETRACAINE WITH MEMBRANES CONTAINING PHOSPHATIDYLCHOLINE AND CHOLESTEROL - A H-2 NMR-STUDY [J].
AUGER, M ;
JARRELL, HC ;
SMITH, ICP .
BIOCHEMISTRY, 1988, 27 (13) :4660-4667
[4]   BIOPHYSICS OF LIPID ASSOCIATIONS .3. QUATERNARY SYSTEMS LECITHIN-BILE SALT-CHOLESTEROL-WATER [J].
BOURGES, M ;
SMALL, DM ;
DERVICHI.DG .
BIOCHIMICA ET BIOPHYSICA ACTA, 1967, 144 (02) :189-&
[5]  
BURSTEIN M, 1970, J LIPID RES, V11, P583
[6]  
CAREY MC, 1984, HEPATOLOGY, V4, P1515
[7]  
COLEMAN R, 1975, BIOCHEM SOC T, V3, P747, DOI 10.1042/bst0030747
[8]   EFFECT OF TEMPERATURE ON CRITICAL MICELLE CONCENTRATION OF SOME PARAFFIN-CHAIN SALTS [J].
FLOCKHART, B .
JOURNAL OF COLLOID SCIENCE, 1961, 16 (05) :484-&
[9]  
HUI SW, 1990, BIOPHYS J, V57, pA469
[10]   EFFECTS OF LIPID PACKING ON POLYMORPHIC PHASE-BEHAVIOR AND MEMBRANE-PROPERTIES [J].
HUI, SW ;
SEN, A .
PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA, 1989, 86 (15) :5825-5829