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 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.
Alkan-Onyuksel
H
H
Department of Pharmaceutics, University of Illinois, College of Pharmacy, Chicago 60612.
Son
K
K
D001798:Blood Proteins / Q000378:metabolism; D002021:Buffers; D055598:Chemical Phenomena; D002627:Chemistry, Physical; D002784:Cholesterol / Q000737:chemistry; D004337:Drug Carriers; D006801:Humans; D006863:Hydrogen-Ion Concentration; D008027:Light; D008081:Liposomes; D008823:Micelles; D010316:Particle Size; D010713:Phosphatidylcholines; D012542:Scattering, Radiation; D013696:Temperature; D013713:Teniposide / Q000008:administration & dosage*
D001798:Blood Proteins; D002021:Buffers; D004337:Drug Carriers; D008081:Liposomes; D008823:Micelles; D010713:Phosphatidylcholines; D013713:Teniposide; D002784:Cholesterol