The compression of water-insoluble drug monolayers spread on the aqueous subphase containing cyclodextrins (CD) led to a shift of surface pressure (pi)-area (A) isotherms toward smaller molecular areas with respect to the pi-A isotherms on the pure water subphase. The displacement of the compression
Drug–Cyclodextrin Association Constants Determined by Surface Tension and Surface Pressure Measurements: I. Host–Guest Complexation of Water Soluble Drugs by Cyclodextrins: Polymyxin B–β Cyclodextrin System
✍ Scribed by Angelina Angelova; Catherine Ringard-Lefebvre; Adam Baszkin
- Publisher
- Elsevier Science
- Year
- 1999
- Tongue
- English
- Weight
- 76 KB
- Volume
- 212
- Category
- Article
- ISSN
- 0021-9797
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✦ Synopsis
The complexation reaction between the amphiphilic peptide antibiotic polymyxin B and naturally occurring cyclodextrins, used as potential drug carriers, was quantitatively evaluated from surface tension measurements at various drug concentrations. The association constant, Ka, of polymyxin B:beta-cyclodextrin inclusion complex formation of 1:1 stoichiometry was determined from the change in the drug interfacial activity upon the addition of beta-cyclodextrin at the excess solution concentration (10(-3) M). The obtained Ka value is discussed in terms of molecular matching of the host cyclodextrin cavity and the guest drug molecule. Copyright 1999 Academic Press.
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