Mixed micelles as proliposomes for the solubilization of teniposide

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 ph...

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Bibliographic Details
Published in:Pharmaceutical research 1992-12, Vol.9 (12), p.1556-1562
Main Authors: ALKAN-ONYUKSEL, H, SON, K
Format: Article
Language:English
Subjects:
Biological and medical sciences
Blood Proteins - metabolism
Buffers
Chemical Phenomena
Chemistry, Physical
Cholesterol - chemistry
Drug Carriers
General pharmacology
Humans
Hydrogen-Ion Concentration
Light
Liposomes
Medical sciences
Micelles
Particle Size
Pharmaceutical technology. Pharmaceutical industry
Pharmacology. Drug treatments
Phosphatidylcholines
Scattering, Radiation
Temperature
Teniposide - administration & dosage
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Summary: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.
ISSN:0724-8741
1573-904X
DOI:10.1023/A:1015804206414