Mixed micelles as proliposomes for the solubilization of teniposide

• 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
• ISSN: 0724-8741; 1573-904X
• 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.