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  • Title: Combined effect of SLS and (SBE)(7M)-beta-CD on the solubilization of NSC-639829.
    Author: Yang G, Jain N, Yalkowsky SH.
    Journal: Int J Pharm; 2004 Jan 09; 269(1):141-8. PubMed ID: 14698585.
    Abstract:
    Complexation and micellization are two effective ways of solubilizing drugs. In this study, the combined effect of surfactant and complexant on the solubilization of a poorly water soluble compound (NSC-639829) is investigated. With increasing concentration of sodium lauryl sulphate (SLS) in solutions of fixed concentration of (SBE)(7M)-beta-CD, the total solubility of the drug decreases linearly, reaches a minimum and then increases linearly. At each minimum, the molar ratio of SLS to (SBE)(7M)-beta-CD is close to unity. The above observation is attributed to the fact that the surfactant molecule competes with the drug to "fit" in the non-polar cyclodextrin cavity. The surfactant depletes cyclodextrin to form a 1:1 complex. Once the concentration of free SLS reaches the CMC, it starts forming micelles and hence, solubilizes the drug. A slight decrease of the solubilizing power is noticed in the presence of SLS/(SBE)(7M)-beta-CD complex. The combined use of two solubilizing agents, a surfactant and a complexant, results in a much lower solubility than when either one is used alone at the same concentration. The surfactant molecule acts as a competitive inhibitor in the solubilization of the drug by the complexant. Similarly the complexant "pulls" the surfactant out of solution, making it unavailable for solubilizing the drug.
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