Combined effect of SLS and (SBE)7M-β-CD on the solubilization of NSC-639829

Gang Yang, Neera Jain, Samuel H Yalkowsky

Research output: Contribution to journalArticle

21 Citations (Scopus)

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-β-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-β-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-β-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.

Original languageEnglish (US)
Pages (from-to)141-148
Number of pages8
JournalInternational Journal of Pharmaceutics
Volume269
Issue number1
DOIs
StatePublished - Jan 9 2004

Fingerprint

N-4-((5-bromo-2-pyrimidoxy)-3-methylphenyl)-(2-dimethylamino)benzoylurea
Surface-Active Agents
Sodium Dodecyl Sulfate
Pharmaceutical Preparations
Cyclodextrins
Solubility
Micelles
Observation

Keywords

  • Combined effect
  • Complexation
  • Micellization
  • NSC-639829
  • Solubilization

ASJC Scopus subject areas

  • Pharmaceutical Science

Cite this

Combined effect of SLS and (SBE)7M-β-CD on the solubilization of NSC-639829. / Yang, Gang; Jain, Neera; Yalkowsky, Samuel H.

In: International Journal of Pharmaceutics, Vol. 269, No. 1, 09.01.2004, p. 141-148.

Research output: Contribution to journalArticle

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